5-HT Receptor

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.

Hymenidin, an alkaloid isolated from the Okinawan sponge Hymeniacidon sp. is a 5-hydroxytryptaminergic receptor antagonist and voltage-gated potassium channel inhibitor with potential antiprotozoal effects.It selectively binds to FOXO1 DNA and reduces depolarization-induced elevation of cellular calcium.

E-3620 is a novel 5-HT3 receptor antagonist that inhibits cisplatin-induced vomiting in beagles. E-3620 can be used to study dyskinesia, gastrointestinal dyskinesia, psoriasis and psoriasis.

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.

Agomelatine (Valdoxan) is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors, tested in an animal model of depression.

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

Homoeriodictyol, a naturally occurring, bitter-masking flavanone, as a promising agent to increase appetite and food intake. The flavanone homoeriodictyol can increase SGLT-1-mediated glucose uptake but decrease serotonin release in differentiated Caco-2 cells.

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

Zatosetron maleate（LY 277359 maleate） is a potent and selective serotonin 5HT3 receptor antagonist for the study of acute migraine.

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.

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

GTS-21 dihydrochloride (DMBX-anabaseine) is a nAChRs agonist. nAChRs are neuron receptor proteins that activated by the binding of the neurotransmitter ACh.

Tandospirone citrate (SM-3997 citrate) is a potent and selective 5-HT1A receptor partial agonist (Ki : 27 nM)

Fluoxetine (LY-110140) is a highly specific serotonin uptake inhibitor and selective 5-hydroxytryptamine (5-HT) reuptake inhibitor. Fluoxetine has antidepressant activity.

Clovoxamine (DU 23811) is a 5-hydroxytryptamine reuptake, serotonin and norepinephrine inhibitor with antidepressant and anticonvulsant activity.

Roxindole (EMD 49980) is a selective dopamine autoreceptor and 5-HT1A dual agonist and inhibitor of 5-hydroxytryptamine (5-HT) uptake with antipsychotic and antidepressant activity.Roxindole can be used to study Parkinson's and neurodivergence.

Osemozotan HCl (Osemozotan hydrochloride) is a novel and selective 5-HT1A receptor agonist that reduces methamphetamine-induced c-Fos expression in the medial prefrontal cortex and striatum.Osemozotan HCl is used in the study of mechanical abnormalities of pain and depression.

OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist with antidepressant-like activity, showing high affinity for the sigma receptor σ1 2 (IC50=47 56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM).

PF-184298 is a serotonin and norepinephrine monoamine reuptake inhibitor (SNRI) that inhibits dopamine reuptake.

BF-1 is a novel selective 5-HT2 receptor antagonist that acts by blocking neurogenic dural plasma protein extravasation induced by mCPP or BW723C86.BF-1 is used in the study of migraine.

SPD-473 citrate (BTS 74398 citrate) is a dopamine reuptake inhibitor, a norepinephrine transporter protein (NET) inhibitor, and a 5-hydroxytryptamine reuptake inhibitor, and is used in the study of neurological disorders and endocrine and metabolic diseases.

Nelotanserin (APD125) is a potent 5-HT2A inverse agonist(IC50 : 1.7 nM), a moderately potent 5-HT2C partial inverse agonist t(IC50 :79 nM )and a weak 5-HT2B inverse agonistt(IC50 : 791 nM).

Liafensine(BMS-820836) is a novel and selective triple monoamine reuptake inhibitor with inhibitory effects on the reuptake of serotonin, norepinephrine, and dopamine for the study of major depressive disorder and central nervous system disorders.

SCH-23390 hydrochloride (R-(+)-SCH23390 hydrochloride) is an effective dopamine receptor antagonist, with high affinity for the D1 (Ki=0.2 nM) and D5 (Ki=0.3 nM) receptors.

BIMU 8 is a selective agonist of 5-HT4 with EC50s of 18 nM, 77 nM, and 540 nM for wild-type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4.

cis-Urocanic acid ((E)-Urocanic acid) is a 5-HT2A receptor agonist (Kd: 4.6 nM). It is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.

Lorcaserin is a selective serotonin agonist that has been recently approved as a weight loss agent.

Quinupramine (LM 208) is an orally available classical tricyclic antidepressant compound with a strong affinity for muscarinic and 5-HT receptors.Quinupramine crosses the central nervous system and can be used in the study of neurologic disorders.

AVN-322 is an orally active and specific 5-HT6R antagonist for the study of CNS disorders such as impaired memory and schizophrenia.

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

EMD 56551 is a selective small molecule 5-HT1A receptor agonist with anxiolytic activity for the study of anxiety disorders.

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

Ebalzotan (NAE 086) is a 5-HT1A receptor agonist that can be used to study depression.

Serotonin (5-hydroxytryptamine) is a natural product from animals

SB-269970 hydrochloride (SB-269970A) , a hydrochloride salt form of SB-269970, is a 5-HT7 receptor antagonist (pKi of 8.3) and exhibits >50-fold selectivity against other receptors.

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

Nemifitide diTFA (INN 00835 diTFA) is a synthetic pentapeptide that can cross the blood-brain barrier and acts as a potent antidepressant, similar to melanocyte suppressor factor (MIF).

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

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.

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

Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties. Amitriptyline is widely used to treat depression and neuropathic pain.

(S)-Mirtazapine ((S)-Org3770) is the S(+)-enantiomer of Mirtazapine, functioning as a selective 5-HT2 receptor antagonist with pro-nociceptive effects. It is commonly used in combination with the R(-)-enantiomer of Mirtazapine to study depression.

SEP-363856 hydrochloride (SEP-856 hydrochloride) is an orally active, CNS-active psychotropic agent with a unique non-D2 5-HT2A mechanism of action, demonstrating antipsychotic-like effects and potential for schizophrenia treatment.

ADR-851 free base (ADR 851 free base) is a 5-HT3 receptor antagonist and a novel antiemetic with analgesic activity.

Pridefine (Pridefina) is a pyrrolidine derivative, a reuptake blocker of catecholamines and serotonin, with antidepressant activity.

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.

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.

Risperidone (R 64 766) is a selective blocker of dopamine D2 receptors and serotonin 5-HT2 receptors that act as an atypical antipsychotic agent.

1. gamma-Mangostin (Normangostin) as a preventive agent of the metabolic syndrome. 2. Gamma-Mangostin has free radical scavenging activity, and antiproliferative and apoptotic activity in HepG2 cells. 3. Gamma-Mangostin could serve as a micronutrient for colon cancer prevention and is a potential lead compound for the development of anti-colon cancer agents. 4. Gamma-Mangostin may acts as an antihypertensive agent , by causing vasorelaxation which is mediated via the NO-cGMP pathway.

Sertraline hydrochloride (Sertraline HCl) is a selective serotonin uptake inhibitor that is used in the treatment of depression.