5-HT Receptor Agonist

Buspirone (Standard) is the analytical standard of Buspirone. This product is intended for research and analytical applications. Buspirone is an orally active 5-HT1A receptor agonist, and a dopamine D2 autoreceptorsant antagonist. Buspirone is an anxiolytic agent, and can be used for the generalized anxiety disorder research.

Quetiapine-d₄ (fumarate) is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects.

DSP-1053, a benzylpiperidine derivative, is a potent Serotonin Transporter (SERT) inhibitor with a K_i of 1.02 nM. DSP-1053 shows partial 5-HT_1A receptor agonistic activity with a K_i of 5.05 nM. DSP-1053 has antidepressant activity.

Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT₄ receptor partial agonist (EC₅₀=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease.

Aripiprazole (1,1,2,2,3,3,4,4-d₈) is the deuterium labeled Aripiprazole. Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a K_i of 4.2 nM.

Eptapirone (F11440) is a potent, selective and orally active 5-HT_1A receptor agonist (pK_i = 8.33). Eptapirone can inhibit cAMP production. Eptapirone can reduce 5-HT levels and increase corticosterone levels. Eptapirone shows potent anxiolytic and antidepressant potential. Eptapirone can be used for the research of neurological disease, such as anxiety and depression.

Naluzotan hydrochloride is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC₅₀ and K_i of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K⁺ channel blocker, with IC₅₀ of 3800 nM.

Bifeprunox mesylate is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pK_is of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC₅₀ of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox mesylate is an antipsychotic for the research of schizophrenia.

Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.

LY334370 fumarate is the fumarate of LY334370 (HY-103107). LY334370 is a selective 5-HT_1F receptor agonist with a K_i of 1.6 nM.

WAY 163909 is an orally active, blood-brain barrier permeable 5-HT2C receptor-selective agonist. WAY 163909 exhibits an EC₅₀ of 8 nM and a K_i of 10.5 nM for h5-HT2C. Instead of triggering apoptosis, WAY 163909 induces anorectic, antipsychotic-like, antidepressant-like, anti-aggressive and anti-compulsive effects. WAY 163909 alleviates ketamine-induced hypothermia, but impairs sexual function at high doses. With rapid antidepressant-like properties, WAY 163909 can be used in research related to obesity, schizophrenia, depression, obsessive-compulsive disorder, and anesthesia-induced hypothermia.

Befiradol (NLX-112) hydrochloride is a highly selective 5-HT₁A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol hydrochloride attenuates sedative agent-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of sedative agent-induced analgesia and sedation in adult rats. Befiradol hydrochloride can be used in studies related to opioid-induced respiratory depression.

Capeserod (SL65.0155 free base) is an agonist for serotonin receptor (5-HT receptor), with a K_i of 0.6 nM for 5-HT₄ receptor. Capeserod enhances expression of phopshorilated cAMP-response element binding protein (p-CREB), vascular endothelium growth factor (VEGF), brain-derived neurotrophic factor (BDNF) and B cell lymphoma-2 (Bcl-2) proteins in hippocampus, and exhibits antidepressant-like efficacy in Wistar rats models.

(Rac)-Rotigotine-d₃ hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT_1AR, a full agonist at 5-HT_1BR and 5-HT_1DR with EC₅₀s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT₇R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models.

LP 12 hydrochloride hydrate is a potent and selective 5-HT7 receptor agonist with a K_i of 0.13 nM. LP 12 hydrochloride hydrate displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (K_i values are 224 nM, 60.9 nM and >1000 nM, respectively).

EMD 56551 is a potent and selective 5-HT1A receptor agonist. EMD 56551 exerts anxiolytic activity.

Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT₄ receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pK_i =9.4) for human 5-HT_4(c) receptors.

Urapidil-d₃ is the deuterium labeled Urapidil. Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.

4-Methylamphetamine hydrochloride is a 5-HT1A receptor agonist that induces hypothermia in rats by binding to the 5-HT1A receptor. Additionally, 4-Methylamphetamine hydrochloride acts on norepinephrine (NE), dopamine (DA), and serotonin (5-HT) transporters to increase the extracellular levels of these neurotransmitters. 4-Methylamphetamine hydrochloride can be used in the study of neurological disorders.