Difference between revisions of "Opioid Notes"

Opium Derivatives

Opium Alkaloids

Thebaine - 6,14 Dimethoxy version of Oxymorphone. Stimulant rather than an analgesic.

Narceine - Bitter, Crystalline, formerly used as a substitute for Morphine.

Noscapine - Acts on the Sigma receptor. Non painkilling. Used commonly in Antitussives. Blocks Bradykinine B-2 receptors in Stroke patients.

Alkaloid Salt Mixtures

Pantopon - Preparation of all alkaloids present in opium without plant matter. Injectable and slightly less potent than Morphine.

Morphine Family

6-MDDM - 80x the potency of Morphine, has a faster onset and less body load then the prior.

Azidomorphine - 40x the potency of Morphine, has a high affinity for μ.

Hydromorphinol - Derivative of Morphine, yet more potent, with a steeper-dose-response curve and a longer half life. Scripted in Sweden.

Methyldesorphin - 15x the potency of Morphine. Is found in some mixtures of Krokodil.

MR-2096 - Oxymorphone analogue that is roughly the same potency.

N-Phenethylnormorphine - 8-14x the potency of Morphine.

RAM-378 - N-Phenethyl analogue of Hydromorphinol. It is probably more potent as a result.

3,6 Morphine Diesters

Diacetyldihydromorphine - Occasionally used as an alternative to diamorphine, of which it is faster acting, longer lasting and has less side effects such as euphoria and addiction. However it is equipotent with Morphine.

Dipropanoylmorphine - Ester of Morphine used to treat severe pain. Rarely used but considered to be safer and less addictive than Morphine. As such carries less side effects, such as euphoria. Slower acting, longer lasting and slightly more potent than Morphine.

Nicomorphone - 2-3x the potency of Morphine and commonly prescribed in German speaking countries.

Codeine-Dionine Family

Heterocodeine - Reverse isomerEach of two or more compounds with the same formula but a different arrangement of atoms in the molecule and different properties. of codeine. 6x the potency of Morphine, while Codeine is a prodrug, Heterocodeine is a direct agonistA substance that initiates a physiological response when combined with a receptor..

Myrophine - Acts as a prodrug to Morphine. Has a slow onset and longer duration, but reduced potency. Does NOT produce addiction or dependence regardless of dose.

Acetyldihydrocodeine - Used in Germany. Close relative of Thebacon, where only the 6-7 cond is unsaturated. 6-Acetyl derivative of Dihydrocodeine. Metabolizes into Dihydromorphine. Higher lipophilicity than codeine. Would probably be more potent and longer lasting as a result. Higher oral BA than Codeine.

Morphinones and Morphols

14-Cinnamoyloxycodeinone - 100x the potency of Morphine.

14-Methoxymetopon - 500x the potency of Morphine. Can be up to one million times the potency of Morphine if injected into the spine.

14-Phenylpropoxymetopon - 2000x potency of Morphine. When injected into the spine up to one million times the potency of Morphine. 14-Methoxymetopon has a ceiling effect on respiratory depression, but the above has been left untested.

3-Acetyloxymorphone - Acetylated analogue of Oxymorphone.

7-Spiroindanyloxymorphone - Odd Oxymorphone analogue that is selective at dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system..

Acetylmorphone - Acetoxy version of Hydromorphone, has a higher bioavailabilityThe fraction of an administered dose that is absorbed into a living system. as a result.

Chloroxymorphamine - Derivative of Oxymorphone and irreversible full agonistA substance that initiates a physiological response when combined with a receptor..

Methyldihydromorphone - Related to Heterocodieine not dihydrocodeine. Is 6-9x the potency of Morphine.

Metopon - Methylated Hydromorphone, less potent. More than likely would have more euphoria as a result.

N-Phenethyl-14-Ethoxymetopon - 60x the potency of Morphine, but produces less constipation. d & u agonistA substance that initiates a physiological response when combined with a receptor..

Oxymorphol - 6-Hydrogenated Oxymorphone.

Pentamorphone - Few times more potent than Fentanyl. Short duration, yet low respiratory depression.

Semorphone - 2 times the potency of Morphine. Partial u agonistA substance that initiates a physiological response when combined with a receptor. and has a ceiling effect on both analgesia and respiratory depression.

Thebacon - Thebaine analogue, that is fairly uninteresting. 6-8x the potency of Codeine.

Hydrazones

Oxymorphazone - Half the potency of Oxymorphone, yet higher doses last up to 48 hours.

Morphians

Butorphanol - partial ant.-ag. at μ opioid and competitive antagonistA substance that interferes with or inhibits the physiological action of another./partial agonistA substance that initiates a physiological response when combined with a receptor. at κ opioid. dysphoria is common at normal dose.

Drotebanol - Morphinan derivative synthesised from Thebaine with analgesic effects several times more potent than codeine but weaker than morphine. Moderately addictive but limited physical dependance. Under Metabanyl when available as a script.

Dextromethorphan (-) - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. / σ1 & σ2 sigma agonistA substance that initiates a physiological response when combined with a receptor. / a3b4, a4b2, a7 nACH antagonistA substance that interferes with or inhibits the physiological action of another., (very weak) μ, δ & κ opioid agonistA substance that initiates a physiological response when combined with a receptor., SERT & NET inhibitor, NADPH Oxidase inhibitor. (Race)Methorphan = racemic

Dextrorphan (-) - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. / σ1 & σ2 sigma agonistA substance that initiates a physiological response when combined with a receptor. / a3b4, a4b2, a7 nACH antagonistA substance that interferes with or inhibits the physiological action of another., L-Type voltage-gated calcium channel (LVGCC) blocker, SRISerotonin Reuptake Inhibitor.

Cyclorphan - mixed antagonistA substance that interferes with or inhibits the physiological action of another.-agonistA substance that initiates a physiological response when combined with a receptor. with affinity for κ

Levophenacylmorphan - 10x potency of M

Levofurethylnormorphanol (Ro4-1539) - potent μ opioid agonistA substance that initiates a physiological response when combined with a receptor. 30-60x potency of Levorphanol.

Levomethorphan (+) - NDMA antagonistA substance that interferes with or inhibits the physiological action of another., σ1 & σ2 sigma agonistA substance that initiates a physiological response when combined with a receptor., μ, δ & κ opioid agonistA substance that initiates a physiological response when combined with a receptor..

Levorphanol (+) - μ, κ & δ agonistA substance that initiates a physiological response when combined with a receptor., 4-8x potency of M, long duration, no cross tolerance with morphine

Norlevorphanol - Opioid analgesic, uninteresting.

Phenomorphan - 10x potency of Levorphanol. :└--> N-(2-(2-furyl)ethyl) analogue - 60x Levorphanol :└--> N-(2-(2-thienyl)ethyl) analogue - 45x Levorphanol

Proxorphan - partial κ agonistA substance that initiates a physiological response when combined with a receptor., lesser partial μ agonistA substance that initiates a physiological response when combined with a receptor.

Ro4-1539 (Furethylnorlevorphanol) - 30-60x the potency of M. One of the more potent u agonists from the Morphans.

(Race)Methorphan: L(eft) (+) Levomethorphan >< Dextromethorphan (-) D(exter) --> l=OPIATE >< d=HALLUCINOGENIC OPIATE

└--> Racemic mix of both isomers, embodying their properties.

Morphinan (Racemorphan): l (+) Levorphanol >< Dextrorphan (-) d --> l=OPIATE >< :d=HALLUCINOGENIC OPIATE

└--> Racemic mix of both isomers, embodying their properties.

(Race)Allorphan: l (+) Levallorphan >< Dextrallorphan (-) d --> l= ANTI-OPIOID >< d=NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. :ANTAGONISTS

└--> Racemic mix of both isomers, embodying their properties.

3-Hydroxymorphinan: l (+) Norlevorphanol >< Nordextrorphan (-) d --> l=OPIATE >< d=NOOTROPIC

└--> Racemic mix of both isomers, embodying their properties.

Oxilorphan: μ antagonistA substance that interferes with or inhibits the physiological action of another. & weak partial κ agonistA substance that initiates a physiological response when combined with a receptor.

Dimemorfan - SIGMAERGIC DRUG

Xorphanol - mixed ant.-ag. produces convulsions at highest dose tested.

Cyprodime - Selective μ opioid antagonistA substance that interferes with or inhibits the physiological action of another. with no affinity for κ or δ receptors

Samidorphan - selective μ antagonistA substance that interferes with or inhibits the physiological action of another.. potential for addiction treatment.

Benzomorphans

Butinazocine - Benzomorphan opioid that was never marketed.

Carbazocine - Benzomorphan opioid that was never marketed.

Etazocine - Partial opioid agonistA substance that initiates a physiological response when combined with a receptor. with mixed ant.-ag. effects. low potency

Ethylketocyclozocine - Partial opioid agonistA substance that initiates a physiological response when combined with a receptor. with mixed ant.-ag. effects.

Ibazocine - Benzomorphan opioid that was never marketed.

Moxazocine - 10x potency of Morphine, partial/mixed ant.-ag.

Tonazocine - Partial agonistA substance that initiates a physiological response when combined with a receptor. at μ & δ, no adverse effects on breathing.

Volazocine - Benzomorphan opioid that was never marketed.

Fluorophen - Radioligand, full μ agonistA substance that initiates a physiological response when combined with a receptor. (6x M) & lower affinity for δ.

Zenazocine - Partial agonistA substance that initiates a physiological response when combined with a receptor. at μ & δ.

Eptazocine - Japanese κ agonistA substance that initiates a physiological response when combined with a receptor. & μ antagonistA substance that interferes with or inhibits the physiological action of another.

Pentazocine - Mixed ant.-ag. (-) is the κ agonistA substance that initiates a physiological response when combined with a receptor. side, the (+) displays 10x the affinity for sigma receptors. NO μ agonism

Phenazocine - Related to ^ but stronger analgesic, 4x potency of M

Cyclazocine - Mixed ant.-ag.

Dezocine - Mixed ant.-ag. with high κ antagonism. Low dose=euphoria (μ) High dose=dysphoria (κ). Weird structure

8-Carboxamidocyclazocine (8-CAC) - κ & μ agonistA substance that initiates a physiological response when combined with a receptor., long duration.

Bremazocine - κ agonistA substance that initiates a physiological response when combined with a receptor. related to Pentazocine

Metazocine - Analgesic; mixed ant.-ag. at μ, activity also at κ and sigma

Alazocine - σ1 agonistA substance that initiates a physiological response when combined with a receptor., κ opioid agonistA substance that initiates a physiological response when combined with a receptor. & slight NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.

4-Phenylpiperidines

4-Fluoropethidine - In comparison to pethidine, it is 50% less potent as an analgesic but 50% more potent as a DRIDopamine Reuptake Inhibitor. (4-iodo & 3, 4-dichloro only increase these differences)

Anileridine - Another banned pethidine analogue, probably abused. Higher analgesia than Meperidine due to n-aminophenyl group and acts withing 15 mins orallyRoute of administration in which the subject swallows a substance., lasting 2-3 hours.

Benzethidine - 4-phenylpiperidine analogue of pethidine. Probably somewhat more potent and euphoric. Never scripted.

Carperidine - fairly normal opiate but unused in medicine and currently LEGAL (08/06/2013)

Furethidine - 4-Phenylpiperidine analogue of pethidine. Probably a lot more potent and abuse prone. Never prescribed.

Morpheridine - related to meperidine but 4x the potency and does not cause convulsions

Phenoperidine - 20-200x the potency of Pethidine. Less hypnotic and than morphine but more emetic (nausea). This can be cured by Haloperidol.

Piminodine - similar dose to M, used in 60's and 70's but was banned. It was probably abused widely

.

Prodines

Alphaprodine - 1.5x Morphine

Allylprodine - Prodine analogue 23x potency of Morphine

Betaprodine - 7.5x Morphine

Prosidol - Russian Prodine analogue

Ketobemidones

Acetoxyketobemidone - Unschedualed analogue of Ketobemidone.

Bemidone - Analogue of Pethidine but significantly less potent, however it has NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonism like Ketobemidone.

Ketobemidone - μ opioid antagonistA substance that interferes with or inhibits the physiological action of another. & NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. More addictive than Morphine.

Others

Loperamide - Peripheral opioid so it cannot cross BBB. useful anti-Diarrhoea med. When used in conjuction with Quinine or Omerprazole can cross BBB and opioid effects are seen.

Picenadol - R isomerEach of two or more compounds with the same formula but a different arrangement of atoms in the molecule and different properties. (or Levopicenadol) is pure μ agonistA substance that initiates a physiological response when combined with a receptor. while S is antagonistA substance that interferes with or inhibits the physiological action of another.. Racemic is mixed that casues low abuse potential but has low κ activity

Open Chain Opioids

Amidones

Dipipadone - Lost Ark of the Covenant.

Phenadoxone - methadone analogue, similar dose to M, lasts 1-4 hours

Levacetylmethadol - Methadone analogue with u agonism and noncompetitive a3b4 NACh antagonism. Brand name Orlaam, prescribed to those unresponsive to methadone or subutex. Long half life (3 days) and heavier affect.

Norpipanone - Was not under international control until case reports of addiction arose.

Isomethadone - Previously used in medicine. μ- δ- agonism. S-isomerEach of two or more compounds with the same formula but a different arrangement of atoms in the molecule and different properties. more potent.

Methadols

Dimepheptanol - Related to Methadone, has two isomers which also have two isomers so 6 possible isomers including racemic.

Moramides

Palfium (Dextomoramide) - 3x potency of M but shorter acting. High BA & fast acting, oral feels like shooting. Low LD50The dosage of a substance at which 50% of the exposed subjects does not survive. To estimate the LD50 for humans, tests are conducted on non-human subjects. & inconsistent potency (one day you may need 5mg, next day 3mg)

Thiambutens

Thiambutenes - Dimethyl-TAB, Diethyl-TAB, Ethylmethyl-TAB. Used in vetinary medicine in Japan. Banned in virtually all countried due to high abuse potential. Anticholinergic and antihistamine properties!

Phenalkoxams

Dextropropoxyphene - Low potency opiate not absorbed by CYP2D6. Also is a potent, noncompetitive α3β4 NACh antagonistA substance that interferes with or inhibits the physiological action of another. and a weak SRISerotonin Reuptake Inhibitor.

Dimenoxadol - Benzillic Acid derivative related to methadone. Banned due to high abuse potential it seems.

Dioxaphetyl butyrate - Banned opioid similar to methadone. Possibly in use or previously in use as a med under the names Amidalgon & Spasmoxal.

Ampromides

Diampromide - Banned Analgesic related to Propiram. Similar potency to M.

Propiram - Slightly more potent than codeine, 3-6hr duration. mixed μ ant.-ag. favouring agonism. affinity for κ & δ, sigma and nmda. 97% oral BA!

Others

IC-26 Methadone analogue with similar potency, but unscheduled.

Lefetamine - Weak opiate on the same scale as codeine but has DRIDopamine Reuptake Inhibitor properties

R-4066 - Methadone analogue with 212x the potency, but a much shorter duration. (3 hours)

Amilidopiperidines

3-Methylfentanyl - 400-6000x potency of M depending on isomerEach of two or more compounds with the same formula but a different arrangement of atoms in the molecule and different properties. (cis-iso more potent)

Alfentanil - 1/4 the potency and 1/3 the duration of fent but 4x quicker onset. The businessman's lunch of opiates.

Betahydroxythiofentanyl - one of the more favoured fent. analogues by addicts, implying euphoria.

Carfentanil - 100x potency of fent., 10000x the potency of M. Used in spetznaz hostage crisis. 10,000x potency of M. Activity in humans starts at 1μg.

Lofentanil - more potent and with a longer duration than carfentanil.

Mirfentanil - fent. analogue with strong selevtivity over μ. Lower doses it antagonises effects caused by lesser opioids but at higher doses is resistant to antagonists, suggesting it has non-opioid mechanisms.

Ohmefentanyl - 6300x morphine at it's most active isomerEach of two or more compounds with the same formula but a different arrangement of atoms in the molecule and different properties.. Analogues of this are even stronger with one possessing 30,000x the potency of M.

Parofluorofentanyl - 150-200x morphine. Sold breifly in 1980.

R-30490 - analogue of carfentanil. Most selective μ agonistA substance that initiates a physiological response when combined with a receptor. of all fentanyl analogues

Remifentanil - Potent ultra short acting fent. analogue. Potency from between 20 and 100ug. Used in medicine as an anaesthetic under Ultiva.

Sufentanil - 5-10x potency of fent

Opipavine Derivatives

7-PET - 300x potency of M, 3-OH derivative is 2200x potency of M. Unscheduled.

Acetorphine - 8700x potency of M

BU-48 - Etorphine derivative. Selective δ agonistA substance that initiates a physiological response when combined with a receptor. and produces only convulsions with slight antidepression.

Buprenorphin - Subutex

Cyprenorphine - Buprenorphine analogue, ant.-ag. effects but with higher affinity towards κ.

Dihydroetorphine -1000-12000x potency of M depending on RoA. Less addictive than other opiates and is used in a similar fashion to Subutex in China.

Etorphine - 1000-3000x potency of M. μ, κ & δ opioid agonistA substance that initiates a physiological response when combined with a receptor.. weak affinity for ORL1 nociceptin/orphanin FQ receptor.

Indoles

18-Methoxycoronaridine - Ibogaine derivative, selective α3β4 nicotinic antagonistA substance that interferes with or inhibits the physiological action of another., however no affinity for α4β2, NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. or seretonin. Retains modest affinity at μ & κ opioid.

7-Hydroxymitragynine - Alkaloid in Kratom. Some 17x potency of M. 30x potency of Mitragynine

Eseroline - Metabolite of the ACh inhibitor physostigmine but potent μ agonistA substance that initiates a physiological response when combined with a receptor.

Hodgkinsine - alkaloid found in Psychotria colorata plants. Has antiviral, antibacterial and antifungal properties. Also μ opioid agonistA substance that initiates a physiological response when combined with a receptor. & NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another..

Ibogaine - Addiction CURE. HT2a agonistA substance that initiates a physiological response when combined with a receptor., κ opioid agonistA substance that initiates a physiological response when combined with a receptor., NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.

Mitragynine - Alkaloid in Kratom. Fairly selective μ agonistA substance that initiates a physiological response when combined with a receptor. but little affinity for δ & κ.

Noribogaine - Metabolite of Ibogaine. Potent SRISerotonin Reuptake Inhibitor, κ antagonistA substance that interferes with or inhibits the physiological action of another., weak μ full agonistA substance that initiates a physiological response when combined with a receptor.

Voacangine - precursor to Ibogine used by iboga plant. Displays similar effects towards addiction as Ibogaine.

Diphenylmethylpiperazines

BW373U86 - Selective δ agonistA substance that initiates a physiological response when combined with a receptor. at 15x stronger affinity. Analgesic and anti-depressant properties along with BDNF release. Produces convulsions at high doses and reverses respiratory depression produced by μ agonism. Also protects heart muscle cells from death during oxygen deprivation, a result of heart attacks.

DPI-227 - highly selective δ agonistA substance that initiates a physiological response when combined with a receptor. with antidepressant effects but produces fewer convulsions than most other dugs in it's family.

DPI-3290 - Potent δ & μ agonistA substance that initiates a physiological response when combined with a receptor. but produces little respiratory depression.

Opioid Peptides

Biphalin - endogenous eptide with high affinity for δ & μ receptors. Potency almost 7x greater than Etorphine and 7000x M. Low side effects; no dependancy caused.

Casomorphins - opiates found in Cow's milk.

DAMGO - synthetic opiate peptide with high μ selectivity. When administered alongside M for 7 days, M had the same effect at the same dose as the first day. I.e. removes tolerance.

Deltorphin - High affinity and selectivity, naturally occuring δ opioid agonistA substance that initiates a physiological response when combined with a receptor..

Dermorphin - South American Tree frog skin. Natural opioid peptide. High potency (30-40x M) and selectivity to μ but may be less likely to cause tolerance and addiction.

Dynorphins - endogenous opioid peptides, primarily k agonists. Useful in the analysis of addiction.

Leu-enkephalin - Endogeneous opioid petide that acts as a δ & μ agonistA substance that initiates a physiological response when combined with a receptor. with strong selectivity for δ.

Met-enkephalin - Opioid Growth Factor (OGF), Endogenous opioid peptide. Primary ligand of the δ receptor along with Leu-enkephalin (high potency and selectivity at δ). Low BA & is metabolised rapidly.

Opiorphin - Endogenous opioid isolated from human saliva.

Others

3-HO-TCP - PCP analogue. More glutamergic than the PCP analogue.

3-HO-BCP - substitutes for both cocaine and morphine at ~5mg (made-up)

AD-1211 - Structure looks unrelated to /most/ other opioid drugs. Mixed AgonistA substance that initiates a physiological response when combined with a receptor.-antagonistA substance that interferes with or inhibits the physiological action of another. at opioid recepts similar to pentazocine. Little to no developement of tolerance/dependence in animal studies.

AH-7921 - Selective μ agonistA substance that initiates a physiological response when combined with a receptor., with 80% potency of M. distributed as an RC, TRs show that it has very little euphoria, indicating euphoria comes from somewhere else. Perhaps sigma? Other opioids are heavily potentiated by it. Perhaps μ agonism is purely analgesic and high comes from a combination of μ & δ with each multiplying the affect of the other. This indicates ultimate opiate high would be moderately selective δ agonistA substance that initiates a physiological response when combined with a receptor.

Azaprocin - Azaprocin - ~10x potency of M. Faster onset and short duration of actin. Discoved in 1963, never been marketed. The derivative subbed on the phenyl ring with a p-nitro group would be more potent by roughly 2.5. (So 25x potency of M) The open ringed 2,6-dimethylpiperazine analouges would also be active.

BRL-52537 - Highly potent and selective κ agonistA substance that initiates a physiological response when combined with a receptor.. Neuroprotective.

Bromadol (BDPC) - 500-10,000x potency of M. Similar to PCP analogues & -HO bonds within them.

C-8813 (Thiobromadol) - 591x potency of M. μ agonistA substance that initiates a physiological response when combined with a receptor. & δ antagonistA substance that interferes with or inhibits the physiological action of another. to reduce repiratory depression. Making the drug safer.

Ciramadol - Opioid related to PCP, Tramadol & Tapentadol. mixed ant.-ag. for μ, low abuse potential and ceiling on respiratory depression.

Enadoline - Highly selective κ agonistA substance that initiates a physiological response when combined with a receptor.. Produces visual distortions, dissociation and of course dysphoria similar to Salvia.

Herkinorin - Analogue of Salvinorin A but the complete opposite. 100x higher μ affinity and 50x lower κ affinity. Also; "does not promote the recruitment of β-arrestin-2 to the intracellular domain of the μ-opioid receptor, or induce receptor internalization". This means Herkinorin may not produce tolerance or dependance.

HZ-2 - κ-opioid agonistA substance that initiates a physiological response when combined with a receptor., same potency as morphine, long duration, high oral BA

ICI-199,441 - high potency, highly selective κ agonistA substance that initiates a physiological response when combined with a receptor. with analgesic effects

Methopholine - Isoquinilone derivative with same efficacy as codeine. Could produces corneal opacity. Analogues are more potent with 4'-nitromethopholine at 20x codeine.

MT-45 - 80% of M. mixed ant.-ag. and mild NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.

Nortilidine - Equipotency of M. Opioid activity is in (1S,2R) iso, NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonism is in (1R,2S) iso. Also acts as a DRIDopamine Reuptake Inhibitor.

O-Desmethyltramadol - metabolite of Tramadol. Considerably more potent than Tramadol. Both (+) & (-) isomers lose SRISerotonin Reuptake Inhibitor function but (-) retains NRI functionality. RC.

Salvinorin A - Highly potent κ agonistA substance that initiates a physiological response when combined with a receptor. and even more potent D2 partial agonistA substance that initiates a physiological response when combined with a receptor.. Use in therapy for addiction.

Salvinorin B ethoxymethyl ether - semi-synthetic analogue of Salv. A. Longer duration @ ~3hrs, active at 50ug & 3000x (!) selectivity over μ & δ

Salvinorin B methoxymethyl ether - Similar to ^^ but less selective. 5x potency as Salvinorin A. Deacetylised from Salvinorin A.

SC-17599 - selective μ agonistA substance that initiates a physiological response when combined with a receptor. with little or no affinity for δ & κ. Potency in between pethidine & morphine.

RWJ-394674 - potent and selective δ agonistA substance that initiates a physiological response when combined with a receptor., however once inside body it is dealkylated to its monodesethyl metabolite RWJ-413216 which is a potent μ agonistA substance that initiates a physiological response when combined with a receptor. with less affinity for δ. δ activity counteracts the respiratory depression the μ causes. Only prominent side effect is sedation (and euphoria!)

TAN-67 - potent and selective δ1 agonistA substance that initiates a physiological response when combined with a receptor.. Has analgesic properties & releases dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system. in the brain. Neuro & cardiac protective properties.

Tapentadol - μ & σ agonistA substance that initiates a physiological response when combined with a receptor. & SNRISerotonin–Norepinephrine Reuptake Inhibitor. Potency in between M & Tram.

Tifluadom - Benzo derivative but without GABAa agonism. Instead selective κ agonism.

U-47700 - Overlays betaprodine, 7.5x morphine.

U-50488 - highly selective κ agonistA substance that initiates a physiological response when combined with a receptor. with analgesic effects

U-69,593 - Potent and selective κ1 agonistA substance that initiates a physiological response when combined with a receptor.. Produces; antinociception, anti-inflammation, anxiolysis (low doses), respiratory depression & diuresis. Also inhibits periphery oxytocin secretion. Not sure if hallucinogenic.

W-15 - 5.4x Morphine. RC.

W-18 - 10,000x potency of M, structure abstract from any other drug. These super potent opioids are used in vetenarian practice for tranquilising elephants.

Opioid Antagonists and Inverse Agonists

(selective δ antagonists may reduce physical addiction without causing w/d if attatched to an opioid)

Chlornaltrexamine - Irreversible mixed ant.-ag. at μ opioid. 22x more potent than M

Cyprodime - Selective μ opioid antagonistA substance that interferes with or inhibits the physiological action of another. with no affinity for κ or δ receptors

Diprenorphine - Strongest opiate antagonistA substance that interferes with or inhibits the physiological action of another. available. 100x potency of Nalorphine. Used to reverse effects of super-potent opioids.

Levallorphan - μ opioid antagonistA substance that interferes with or inhibits the physiological action of another., when used with opiate, it potentiates it and removes addiction potential or induces withdrawal in addicts.

Nalbuphine - mixed ant.-ag. as is common with this class, there occurs analgesia with no addictive properties.

Naloxazone - Irreversible μ opioid receptor antagonistA substance that interferes with or inhibits the physiological action of another.

Naloxonazine - Very Potent Irreversible μ opioid antagonistA substance that interferes with or inhibits the physiological action of another.. dimerizes from Naloxazone under acidic conditions

Naltrexone - Competitive antagonistA substance that interferes with or inhibits the physiological action of another. at μ & κ receptors, and to a lesser extent, δ. Modulation of the dopaminergic mesolimbic pathway makes it good for countering alcohol dependance as well as Opiate addiction. Blocks the euphoric effects of opioids and is used in rapid detoxification and attenuation of withdrawal. If opiates are used simultaneously, oD may occur.

Samidorphan - selective μ antagonistA substance that interferes with or inhibits the physiological action of another.. potential for addiction treatment.

Uncategorised Opioids

FE 200665 - Is an all D-Amino acid peptide that acts as a restucted K-opioid receptor agnoist. Was dosed at 0.36mg/kg IV. Was compared to 15mg oxycodone. Slightly less than the potency of hydrocodone. Caused Hyperalgesic response in a skin pinch test. Also known as CR665.

SoRI-9409 - mixed μ agonistA substance that initiates a physiological response when combined with a receptor. & δ antagonistA substance that interferes with or inhibits the physiological action of another.. moderate analgesia without development of tolerance. Anti-addictive effects for all dopaminergic drugs.

Synthetic Conotoxin - Snail toxin derived painkiller 1000x potency of morphine. Non-addictive

RELATED COMPOUNDS

Amiphenazole - treatment for OD. counteracts respiratory depression. If Morphine-N-oxide is taken on this, M's potency will increase.

Chitosan - linear polysaccharide that can give Morphine up to 60% BA intranasally. Powdered & the ratio is 1.3g : 6.7g (morpine : chitosan)

BIMU-8 - NOOTROPIC

NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonists - Inhibit development of tolerance to morphine

Tezampanel - ANXIOLYTIC

Ibudilast - NOOTROPIC

Nuciferine

Tetrahydropalmatine - ANXIOLYTIC

Lofexidine - ANXIOLYTIC

d & l Phenylalanine (DLPA) - Increases dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system. and endorphin levels, reducing opiate tolerance and even providing an analgesic effect of it's own.

CCK Antagonists

Proglumide - Acts as a d opioid agonistA substance that initiates a physiological response when combined with a receptor. and non selective CCK antagonistA substance that interferes with or inhibits the physiological action of another..Enhances analgesia produced by opioids and can prevent or even reverse the development of tolerance

Devazepide - No affinity for GABAa, selective CCKa antagonistA substance that interferes with or inhibits the physiological action of another..

Lorglumide - Selective CCKa antagonistA substance that interferes with or inhibits the physiological action of another. for treatment of gastrointestinal problems and some forms of cancer as well as Opioid interacting properties.

Nocieceptinergic Drugs

(ORL-1 ant. & ag.'s)

J-113,397 - Highly selective ORL-1 antagonistA substance that interferes with or inhibits the physiological action of another.. Prevents development of opiate tolerance, stimulates dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system. release, cognitive enhancer

SB-612,111 - Selective ORL-1 antagonistA substance that interferes with or inhibits the physiological action of another. but several times the potency of ^^

MCOPPB - Potent, selective ORL-1 agonistA substance that initiates a physiological response when combined with a receptor. with only moderate affinity for μ, even less for δ & κ. Anxiolytic with no inhibition of memory, motor function or sedation

NNC 63-0532 - Potent, selective ORL-1 agonistA substance that initiates a physiological response when combined with a receptor..

Ro64-6198 - Potent, selective ORL-1 agonistA substance that initiates a physiological response when combined with a receptor. with 100x selectivity over others. In rats produced anxiolytic but no anticonvulsant effects. Impairs Short term memory & increases appetite. Reduces analgesic effects of M but no preventing tolerance. In primates it showed analgesic behaviour without respiratory depression.

Menabitan - potent cannabinoidChemicals produced naturally that bind to cannabinoid receptors. They are involved in a variety of mental and physical processes, including pain regulation, food intake, and reward. receptor agonistA substance that initiates a physiological response when combined with a receptor. with anti-nociceptive effects

Enkephalin Potease Inhibitors

RB-101*** - Inhibits enzymes responsible for breaking down enkephalin (regulates nociceptin). Weak μ & δ affinity and slight σ1. Potentiates opiates, stops withdrawal symptoms, no addiction potential, produces no respiratory depression. Also exerts very potent antidepressant and anxiolytic effects. Not orallyRoute of administration in which the subject swallows a substance. active so analogues vv were developed.

RB-120 - Orally active version of the above.

RB-3007 - Another Enkeph. PI & Nociceptin antagonistA substance that interferes with or inhibits the physiological action of another.

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