5-HT Receptor

Ritanserin (R 55667) is a highly effective, relatively selective, long-acting antagonist of 5-HT2 receptor (IC50: 0.9 nM), less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.

Pimavanserin tartrate (Nuplazid) is an effective and specific serotonin 5-HT2A inverse agonist (pIC50: 8.73), used in the therapy of psychosis associated with Parkinson's disease.

Capeserod is a potential 5-HT4 receptor (5-hydroxytryptamine receptor 4) agonist for the study of digestive disorders and neurological disorders.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

AVN-101 is a potent 5-HT7 receptor antagonist.

Dopamine hydrochloride (ASL279) is a naturally occurring catecholamine formed by decarboxylation of dihydroxyphenylalanine and a precursor of norepinephrine and epinephrine. Dopamine hydrochloride binds to alpha-1- and beta-1- adrenergic receptors.

Ziprasidone hydrochloride monohydrate (CP 88059) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of the antipsychotic activity.

L-(R,S)-Tetrahydropalmatine (Rotundine) is extracted from Corydalis yanhusuo W. T. Wang.

Tianeptine (Tianeptine sodium) is a selective 5-HT uptake facilitator in vitro and in vivo.

Mianserin hydrochloride (Org GB 94) is a tetracyclic compound with antidepressant effects. it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. It may cause drowsiness and hematological problems.

Aripiprazole (OPC-14597) is an antipsychotic agent that is structurally related to piperazines and quinolones. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A.

dopamine D1 receptor antagonist

Fluoxetine hydrochloride (Lilly110140) is the first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

LY 272015 hydrochloride is an orally active and selective 5-HT2B receptor antagonist that displays antihypertensive effects in DOCA-salt hypertensive rats.LY 272015 hydrochloride inhibits 5-HT- or BW723C86-induced ERK2 phosphorylation and attenuates MVIC and Tissue downstream cellular effects of 5HT signaling and can be used to study hepatocellular carcinoma.

Trazodone hydrochloride (Trazodone HCl) is a serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety.

Dapoxetine hydrochloride (LY-210448 hydrochloride) is a selectivity short-acting serotonin reuptake inhibitor, used for the therapy of premature ejaculation.

Lesopitron HCl is a 5-HT1A receptor agonist with anxiolytic effects that reverses dark avoidance behavior associated with cocaine withdrawal in mice.

Vilazodone (SB659746A) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and a 5-HT-1A receptor partial agonist, with antidepressant and anti-anxiety activities. Vilazodone inhibits the reuptake of serotonin from the synaptic cleft while stimulating the release of 5-HT into the synaptic cleft. This increases the concentration of 5-HT in the synaptic cleft and potentiates serotonergic neurotransmission in the central nervous system.

Cannabigerol is a high affinity α±2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist ; also binds to the CB2 receptor; it can relieve interocular pressure, which may be of benefit in the treatment of glaucoma.

Faxeladol, a potent adrenergic absorption inhibitor and serotonin reuptake inhibitor, is a small-molecule Opioid receptor agonist that can be used to study neurological disorders.

Lintopride HCl is a 5HT-4 antagonist.

L-745870 trihydrochloride is a highly potent and selective D4 dopamine receptor antagonist.

5-HT7 agonist 1 (4-[4-[(2-chlorophenyl)methyl]piperazin-1-yl]-1H-indole) is a selective agonist of 5-HT7 (IC50 = 222.93 nM). 5-HT7 agonist 1 can be used in studies about CNS disorders.

Landipirdine (RO-5025181) is a selective 5-HT6R antagonist for the study of central nervous system disorders such as dementia.

Org-13011 fumarate1 is an agonist of the 5-HT1A receptor and can be used to study neurological disorders.

(4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist that shows antihypertensive and antiplatelet aggregation activity in hypertensive rats.

Pancopride（LAS 30451） is a novel, orally available, long-acting, selective 5-HT3 receptor antagonist that blocks nitrogen mustard and dacarbazine-induced vomiting.

PRX933 hydrochloride (GW876167 hydrochloride) is an agonist of 5-HT2C receptor and can be used in studies about hypertension acute treatment.

SLV-310 is a potent dopamine D2 receptor antagonist and 5-HT reuptake receptor inhibitor used in the study of neurological disorders such as bipolar disorder and schizophrenia.

Enciprazine (D-3112) has anxiolytic activity with high affinity for 5-HT1A receptor and ADRA1, which can be used for the treatment of anxiety disorders and can be used to study depression.

SB 699551 dihydrochloride is a 5-ht5a receptor antagonist.

MM 77 dihydrochloride is an effecitve 5-HT1A receptor postsynaptic antagonist with anxiolytic-like activity.

Tabernanthalog (TBG) is a 5-HT2A agonist. In rodents,Tabernanthalog has been found to promote structural neuroplasticity, reduce alcohol-seeking and heroin-seeking behavior, and produce antidepressant effects.

(+)-OSU 6162 (Piperidine, 3-[3-(methylsulfonyl)phenyl]-1-propyl-, (3R)-) is an agonist of 5-HT Receptor with anti-Alzheimer and antidepressant activities.

RS 42358-197 (RS 25259-007) is a competitive 5-HT3 receptor antagonist.

Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).

DA-6886 is an agonist 5-Hydroxytryptamine receptor 4 (5-HT4). DA-6886 induced relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels revealed that it inhibited hERG channel current with an pIC50 value of 4.3, indicating that the compound was 1000-fold more selective for the 5-HT4 receptor over hERG channels.

LY-2624803 is a 5-HT2A receptor antagonist and histamine receptor inverse agonist that can be used to improve slow wave sleep.

SB 258585 is a selective 5-HT6 receptor antagonist.SB 258585 has a high affinity for individual receptor populations in cell lines with human recombinant 5-HT6 receptors.SB 258585 can be used to label both recombinant and natural 5-HT6 receptors, and can be used to assay cognitive enhancement and antipsychotic activity.

Lensiprazine (SLV314) is a potent dopamine D(2) receptor antagonist that acts as a serotonin reuptake inhibitor , and can be used to study bipolar disorder and schizophrenia.

5HT6-ligand-1 is an orally active ligand of 5-HT6 receptor (Ki = 1.43 nM).

Rilapine (Rilapinum) is an antipsychotic compound that shows high affinity for 5-HT6 receptors and can be used to study neurological disorders.

Abaperidone is a potent 5-HT2A receptor and dopamine D2 receptor antagonist with an IC50 of 6.2 for 5-HT2A receptors and 17 nM for dopamine D2 receptors.Abaperidone is a potentially atypical anti-psychotropic compound that reduces basal hsp70 mRNA expression in rat striatum and prefrontal cortex. expression in the striatum and prefrontal cortex of rats.

Ricasetron (Brl 46470) is a 5-HT3 receptor antagonist with pro-axonal lysis and antiemetic properties, and is used in the study of anxiety and anxiety disorders.

CP 96021 is a group of 5-HT1 receptors and 5-HT2 receptors antagonists that have anti-inflammatory properties and are non-non-self anti-ulcer compounds for the treatment of gastrointestinal tract and respiratory asthma.

S 16924 is a 5-HT 1A agonist with potential anxiolytic effects and may be useful in the study of neurologic disorders.

Binospirone (MDL 73005EF) is a 5-HT1A receptor agonist with anxiolytic activity used in the study of glaucoma and movement disorders associated with neurologic dysfunction.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

Donitriptan hydrochloride (Donitriptan monohydrochloride) is a potent, high efficacy agonist of 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively