5-HT1 NON-SELECTIVE

Bromocriptine - D1, 2 & HT 1, 2 AgonistA substance that initiates a physiological response when combined with a receptor. RU-24,969 - Selective HT1A & B AgonistA substance that initiates a physiological response when combined with a receptor. Indorenate - Anxiolytic HT AgonistA substance that initiates a physiological response when combined with a receptor. 1A,B 2C


5-HT1a

This receptor is involved in neuromodulation. Agonists decrease heart rate and blood pressure, release NorepinephrineNorepinephrine, or noradrenaline, is a catecholamine with multiple roles including as a hormone and a neurotransmitter. and show efficacy in anxiolysis, antidepression, analgesia and antiemetic effects, the latter two via inhibition of the NK1 receptor (Neurokinin 1). Agonism also causes serotoninA monoamine neurotransmitter, biochemically derived from tryptophan, that is primarily found in the gastrointestinal (GI) tract, platelets, and central nervous system (CNS) of humans and animals. It is a well-known contributor to feelings of well-being. modulation and vice versa; SRISerotonin Reuptake Inhibitor's, SRA's and MOAI's activate the HT1a receptor. DopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system. release has also been found upon agonism of HT1a, contradictory to this however, agonism impairs certain aspects of memory and learning by inhibiting the release of glutamate and acetylcholine, thus some antagonists such as lecozotan have been shown to be novel treatments for Alzheimer's. Other effects of 5-HT1a activation include; Decreased aggression, Increased sociability, Decreased impulsivity, Inhibition of drug-seeking behavior, Facilitation of sex drive and arousal, Inhibition of penile erection, Diminished food intake, Prolongation of REM sleep latency and Reversal of opioid-induced respiratory depression. Has also been shown to interact with BDNF, whether increasing or decreasing it's expression within the brain.


4-Fluoro-5-MeO-DMT* - Potent HT1A agonistA substance that initiates a physiological response when combined with a receptor. - (Tryptamine) 5-CT - Nonselective, high affinity full agonistA substance that initiates a physiological response when combined with a receptor. at HT1A, B, D, 5A and 7 receptors, as well as at HT2, 3 and 6 with lower affinity. Negligible affinity for HT1E & 1F. It binds strongest to HT1A however. 8-OH-DPAT - HT1A, 7 agonistA substance that initiates a physiological response when combined with a receptor. & SRISerotonin Reuptake Inhibitor/RA possesses antidepressant, anxiolytic, serenic, anorectic, antiemetic and analgesic effects. Could remove muscle tension effects from psychedelics through HT7 agonim. (Aminotetraline) Alnespirone - Selective HT1A full agonistA substance that initiates a physiological response when combined with a receptor. (Azapirone) Bay R 1531 - selective HT1A agonistA substance that initiates a physiological response when combined with a receptor. (closed ring 5-MeO-DPTDipropyltryptamine or Quartamine analogue) Bifeprunox - D2 & HT1A agonistA substance that initiates a physiological response when combined with a receptor. Buspirone - HT1A, D2, 3, 4 & a1 agonistA substance that initiates a physiological response when combined with a receptor. (Azapirone) CBDCannabidiol - Low affinity for CB1 & 2, indicating antagonistic action for other agonists. Inverse agonistA substance that initiates a physiological response when combined with a receptor. of CB2, anatgonist of GPR55, HT1a agonistA substance that initiates a physiological response when combined with a receptor. and allosteric modulator of u & d opioid receptros. Multiple isomers exist, possibly lowering or raising some receptor affinities. Ebalzotan - Selective HT1a agonistA substance that initiates a physiological response when combined with a receptor.. Interesting structure. Eptapirone (F-11,440) - Very potent, highly selective HT1a agonistA substance that initiates a physiological response when combined with a receptor.. Human trials produced at an oral dose of 1.5 mg a reduction of body temperature, suppression of REM sleep, increase in cortisol and growth hormone levels with an increase in euphoria and intoxication. Peaks within 30–60 minutes with a total duration of three hours. F-15,599 - Analogue of Eptapirone ^^ with similar affect. Ginkgo Biloba - Reversible, nonselective MAOIMonoamine oxidase inhibitor are drugs that inhibit the action of monoamine oxidase in the brain and so allow monoamines to accumulate., Triple RI and selective HT1a agonistA substance that initiates a physiological response when combined with a receptor.. Lecozotan - Competitive, selective HT1A antagonistA substance that interferes with or inhibits the physiological action of another., which enhances the Po-stimulated release of ACh and glutamate. LY-293,284* - Potent selective HT1A full agonistA substance that initiates a physiological response when combined with a receptor. derived from LSD and Bay R 1531. NBUMP - Highly selective HT1A agonistA substance that initiates a physiological response when combined with a receptor. over a1 & D2 receptors. Nefazodone - AD; potent HT2a antag. with low affinity for a1&2 adren., HT1a and D2. Low affinity for SERT, DAT & NET acting as weak SNDRISerotonin–Norepinephrine–Dopamine Reuptake Inhibitor. Osemozotan - HT1A agonistA substance that initiates a physiological response when combined with a receptor. RU-24,969 - Selective HT1A & B AgonistA substance that initiates a physiological response when combined with a receptor. U-92,016-A - Potent, selective full HT1a agonistA substance that initiates a physiological response when combined with a receptor. with a long duration of action. Interesting structure. Umespirone - HT1A & D2 agonistA substance that initiates a physiological response when combined with a receptor., a1 antagonistA substance that interferes with or inhibits the physiological action of another.. Weak affinity for sigma receptor. (Azapirone


HT1B

In the frontal cortex it is responsible for inhibiting the release of dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system., in the basal ganglia and striatum, 5-HT inhibits the release of serotoninA monoamine neurotransmitter, biochemically derived from tryptophan, that is primarily found in the gastrointestinal (GI) tract, platelets, and central nervous system (CNS) of humans and animals. It is a well-known contributor to feelings of well-being. and decreases glutamatergic transmission and in the Hippocampus it produces a facilitation in excitatory synaptic transmission which is altered in depression. Outside the brain, activation can cause pulmonary vasoconstriction. Knockout mice lacking the 5-HT1B gene show an increase in aggression and a higher preference for alcohol.


CP-94,253 - Potent and selective HT1b agonistA substance that initiates a physiological response when combined with a receptor.. Promotes wakefulness, antidepression and enhances cocaine by increasing dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system. release. SB-216,641 - Selective HT1b antagonistA substance that interferes with or inhibits the physiological action of another., has anxiolytic properties.


HT1D

Acts on the CNSCentral Nervous System and affects locomotion and anxiety. It also induces vascular vasoconstriction in the brain.

5-(Nonyloxy)tryptamine - Selective HT1d agonistA substance that initiates a physiological response when combined with a receptor. (1.0nM) BRL-15,572 - Selective HT1d antagonistA substance that interferes with or inhibits the physiological action of another. useful in finding the role of HT1d. HT1d seems to modulate release of glutamate and regulates cerebral blood pressure, making agonists effective migraine cures.


HT1E

Function UNKNOWN. Hypothesised that it plays a large role in regulation of memory. This receptor is also not found in animals.

BRL-54443 - Selective agonistA substance that initiates a physiological response when combined with a receptor. for HT1e & f. Only known (partially) selective ligand.


HT1F

Lasmiditan - Selective HT1f agonistA substance that initiates a physiological response when combined with a receptor. used in treatment of migraines. Lack of affinity for other receptors like HT1b&d may result in fewer vasoconstriction related side effects


5-HT2

5-APB - MDA analogue. Triple RI, HT2 agonistA substance that initiates a physiological response when combined with a receptor. with selectivity over 2B & C (PhenethylaminePhenethylamine (PEA) is a natural monoamine alkaloid, trace amine, and psychoactive drug with stimulant effects. In the mammalian central nervous system, phenethylamine is believed to function as a neuromodulator or neurotransmitter.) 5-MAPB - Similar to ^^ but MDMA analogue (PhenethylaminePhenethylamine (PEA) is a natural monoamine alkaloid, trace amine, and psychoactive drug with stimulant effects. In the mammalian central nervous system, phenethylamine is believed to function as a neuromodulator or neurotransmitter.) 6-APB - MDA analogue. Triple RI, HT2 agonistA substance that initiates a physiological response when combined with a receptor. with selectivity for 2B (PhenethylaminePhenethylamine (PEA) is a natural monoamine alkaloid, trace amine, and psychoactive drug with stimulant effects. In the mammalian central nervous system, phenethylamine is believed to function as a neuromodulator or neurotransmitter.) 6-MAPB - Similar to ^^ but MDMA analogue (PhenethylaminePhenethylamine (PEA) is a natural monoamine alkaloid, trace amine, and psychoactive drug with stimulant effects. In the mammalian central nervous system, phenethylamine is believed to function as a neuromodulator or neurotransmitter.) Medifoxamine - DRIDopamine Reuptake Inhibitor & HT2A & C agonistA substance that initiates a physiological response when combined with a receptor.. hepatotoxic. Oxaflozane - HT1A,2A,2C AgonistA substance that initiates a physiological response when combined with a receptor. Synephrine - strong a1 agonistA substance that initiates a physiological response when combined with a receptor., non selective adrenergic and HT2A



HT2A

HT2A agonism doesn't automatically mean the compound will be psychedelic. 6-Fl-DETDiethyltryptamine is inactive as a psychedelic despite agonising HT2a. The same occurs in Lisuride, an ergoloid derivative. Lisuride has high affinity for D2,3&4, HT1a,2a&c but lacks psychedelic affect. This suggests that there are various genes (GPCR oligomers) encoded into the HT2a receptor and while a less selective ligand such as LSD can connect with these receptors (specifically MGluR-2), some cannot and display no psychedelic effects. This suggests that in future, compounds will be able to access these more selective sites to shape the affect of the drug.


HT2B

- CNSCentral Nervous System Presynaptic Inhibition - meaning agonism causes serotoninA monoamine neurotransmitter, biochemically derived from tryptophan, that is primarily found in the gastrointestinal (GI) tract, platelets, and central nervous system (CNS) of humans and animals. It is a well-known contributor to feelings of well-being. to be released. HT2B inhibited mice were void of MDMA-induced hyperlocomotion and 5-HT release. - Pulmonary vasoconstriction - agonism caused - HT2B regulates cardiac function. In failing human heart conditions, HT2B receptors were way overexpressed than usual. - Modulates serotoninA monoamine neurotransmitter, biochemically derived from tryptophan, that is primarily found in the gastrointestinal (GI) tract, platelets, and central nervous system (CNS) of humans and animals. It is a well-known contributor to feelings of well-being. release and protects against serotoninA monoamine neurotransmitter, biochemically derived from tryptophan, that is primarily found in the gastrointestinal (GI) tract, platelets, and central nervous system (CNS) of humans and animals. It is a well-known contributor to feelings of well-being. syndrome even if agonised.


HT2C

Significantly regulate mood, anxiety, feeding and reproducing by regulating dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system. release in multiple areas of the brain. Antagonism increases dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system. release however. Therefore the agonism of HT2C contributes to depression and anxiety. In fact suicide victims usually have an abnormally high amount of HT2C receptors present in the prefrontal cortex.


HT3

Full agonism however causes nausea and vomiting, anxiety and higher propensity of seizure rate. Similarly full antagonism causes convulsions and anxiety. Agonists also produce nociceptinergic excitation, possibly having effects of addiction and withdrawal.

RS-56812 - Potent and selective partial HT3 agonistA substance that initiates a physiological response when combined with a receptor.. Memory enhancer. YM-31636 - Selective HT3 agonistA substance that initiates a physiological response when combined with a receptor., increases colonic mobility but does not induce diarrhea.

Ondanestron - Selective HT3 antagonistA substance that interferes with or inhibits the physiological action of another. used as an antiemetic for cancer patients. While having no affinity for any other D or HT receptors, Ondanestron has proved useful in treating schizophrenia. It also has found use as withdrawal and craving reducer for alcohol and opioids. Thujone - Active ingredient in Absinthe. Acts as a HT3 antagonistA substance that interferes with or inhibits the physiological action of another. and GABAGamma aminobutyric acid an amino acid that is found in the central nervous system; acts as an inhibitory neurotransmitter.-A antagonistA substance that interferes with or inhibits the physiological action of another., resulting in convulsions and paranoia.


HT-4

Indeloxazine* - S releaserA releasing agent (RA), or simply releaser, is a drug that induces the release of a neurotransmitter from the presynaptic neuron into the synapse, leading to an increase in the extracellular concentrations of the neurotransmitter., DRIDopamine Reuptake Inhibitor, NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antag., acetylcholine releaserA releasing agent (RA), or simply releaser, is a drug that induces the release of a neurotransmitter from the presynaptic neuron into the synapse, leading to an increase in the extracellular concentrations of the neurotransmitter. PRX-03140 - Partial HT4 agonistA substance that initiates a physiological response when combined with a receptor. developed for Alzheimer's. RS-67,333 - Potent partial HT4 agonistA substance that initiates a physiological response when combined with a receptor. as well as being a sigma-1 ligand. Possesses antidepressant and nootropicNootropics, also referred to as smart drugs, memory enhancers, neuro enhancers, cognitive enhancers, and intelligence enhancers, are drugs, supplements, nutraceuticals, and functional foods that purportedly improve mental functions such as cognition, memory, intelligence, motivation, attention, and concentration. They are generally neuroprotective, and non-toxic. properties. SL65.0155 * - Selective partial HT4 agonistA substance that initiates a physiological response when combined with a receptor.. Enhances cognition, learning, memory and has antidepressant effects. Was in phase II trials then abandoned??


HT-5a

5-HT5b is non functional in humans HT-5a functions as an agonistA substance that initiates a physiological response when combined with a receptor. by negatively influencing cAMP levels via Giα & Goα receptors.

SB-699,551 - Potent and selective HT5A antagonistA substance that interferes with or inhibits the physiological action of another. used to decipher the role of HT5A in humans. It seems to modulate serotoninA monoamine neurotransmitter, biochemically derived from tryptophan, that is primarily found in the gastrointestinal (GI) tract, platelets, and central nervous system (CNS) of humans and animals. It is a well-known contributor to feelings of well-being. release similar to HT1b & d.


HT-6

HT-6 blockade causes increased glutamergic and cholinergic neurotransmission, while activation enhances GABAergic signalling.

EMD-386,088 - Potent and selective HT6 agonistA substance that initiates a physiological response when combined with a receptor., however has moderate affinity for HT3. EMDT - Selective HT6 agonistA substance that initiates a physiological response when combined with a receptor.. Inhibits both short and long term memory formation.

Lu AE58054 - Potent and selective HT6 antagonistA substance that interferes with or inhibits the physiological action of another., responsible for memory formation and has use for patients with Alzheimer's and schizophrenia MS-245 - Tryptamine derivative that acts as a selective HT6 antagonistA substance that interferes with or inhibits the physiological action of another.. Boosts the effects of amphetamine and nicotine. PRX-07034 - Potent, selective HT6 antagonistA substance that interferes with or inhibits the physiological action of another., improving cognitive function and anoretic capabilities. SB-742,457 * - Potent, selective antagonistA substance that interferes with or inhibits the physiological action of another. of HT6, with cognition, memory and learning enhancing effects. Currently under phase II trials.


5-HT7

The HT-7 receptor is coupled with the Gs proteines, stimulating cAMP levels. It also plays a role in smooth muscle relaxation within the vasculature and in the gastrointestinal tract. As a result the HT-7 receptor is involved with thermoregulation, circadian rhythm, learning and memory, sleep and mood regulation.

AS-19 - potent HT7 agonistA substance that initiates a physiological response when combined with a receptor. associated with long term memory. Revereses amnesia induced by drugs such as scopolamine and dizocilpine and improves long term memory acquisition, but inhibits short term memory formation. E-55888 - Potent, selective HT7 agonistA substance that initiates a physiological response when combined with a receptor., when administered alongside morphine it was found to significantly increase analgesic effects N-Methylserotonin - Selective and high affinity HT1a & 7 agonistA substance that initiates a physiological response when combined with a receptor., while also functioning as an SSRISelective Serotonin Reuptake Inhibitor. RA-7** - 1-(2-Diphenyl)piperazine. Potent and selective HT7 agonistA substance that initiates a physiological response when combined with a receptor.. Similar in struture to such compounds as 2-DPMP and PCP.

SB-258,719 - Potent, selective HT7 antagonistA substance that interferes with or inhibits the physiological action of another. (or Inverse agonistA substance that initiates a physiological response when combined with a receptor.). Potential for use as an analgesic but also include treatment for anxiety, depression and usage as a nootropicNootropics, also referred to as smart drugs, memory enhancers, neuro enhancers, cognitive enhancers, and intelligence enhancers, are drugs, supplements, nutraceuticals, and functional foods that purportedly improve mental functions such as cognition, memory, intelligence, motivation, attention, and concentration. They are generally neuroprotective, and non-toxic..


NON-SELECTIVE

CSP-2503 * - Potent and Selective HT1a agonistA substance that initiates a physiological response when combined with a receptor., HT2a and HT3 antagonistA substance that interferes with or inhibits the physiological action of another.. Produces anxiolytic effects and potential substance addiction cure. EGIS-12,233 - Potent and selective HT6&7 antagonistA substance that interferes with or inhibits the physiological action of another., increases dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system. within cochlear tissue indicating a role in regulation of the hearing system. TFMPP - Full agonistA substance that initiates a physiological response when combined with a receptor. at HT1a, b, d and 2c, partial agonistA substance that initiates a physiological response when combined with a receptor. or antagonistA substance that interferes with or inhibits the physiological action of another. at 2a. Also binds to SERT and evokoes the release of serotoninA monoamine neurotransmitter, biochemically derived from tryptophan, that is primarily found in the gastrointestinal (GI) tract, platelets, and central nervous system (CNS) of humans and animals. It is a well-known contributor to feelings of well-being.. Adatanserin - Mixed HT1a partial agonistA substance that initiates a physiological response when combined with a receptor. and HT2a & c antagonistA substance that interferes with or inhibits the physiological action of another.. Neuroprotective against ischemia-induced glutamatergic excitotoxicity. (Ischemia = restriction of blood supply to tissues)

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