5-HT Receptor Agonist

Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist that can cross the blood-brain barrier, with K_is of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine.

SEP-363856 (SEP-856) hydrochloride, an orally active TAAR1 and 5-HT1A agonist and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride has the potential for the study of schizophrenia.

5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action.

IHCH-7086 is a blood-brain barrier-permeable, partial β-arrestin-biased agonist of 5-HT_2AR with a K_i of 12.59 nM. IHCH-7086 blocks D-lysergic acid diethylamide-induced head-twitch response in mice and alleviates depression-like behaviors in mice subjected to acute restraint stress or injected with Corticosterone (HY-B1618). IHCH-7086 is applicable to research related to depression.

TCB2 is an agonist of serotonin 5-HT_2A receptor.

LY 344864 is a selective, orally active 5-HT_1F receptor agonist with a K_i of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent.

Tandospirone (SM-3997) is a potent and selective 5-HT_1A receptor partial agonist, with a K_i of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms.

Parishin C is a brain-penetrant major bioactive component found in Gastrodia elata Blume. Parishin C is a 5-HT1A receptor agonist with an EC₅₀ of 34 nM. Parishin C has antipsychotic and neuroprotective effects. Parishin C protects against Aβ-induced long-term potentiation damage and NMDA receptor current impairment. Parishin C reduces oxidative stress, pro-inflammatory cytokine levels, caspase activity, brain water content, and cerebral infarct volume; increases antioxidant enzyme activity and BDNF levels; improves nerve function and histopathological brain damage. Parishin C attenuates phencyclidine-induced immobility time increases, sociability deficits, and visual recognition memory impairment. Parishin C can be used for the research of ischemic stroke, Alzheimer's disease, and schizophrenia-like psychosis.

Eletriptan hydrobromide (Eletriptan HBr) is a 5-HT_1B and 5-HT_1D receptor agonist with antimigraine activity, with K_i of 0.92 nM and 3.14 nM, respectively.

(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT_2C receptor agonist with a K_i of 4 nM and an EC₅₀ of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT_2C than 5-HT_2A and 5-HT_2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects.

Mosapride is an orally active gastroenterokinetic compound. Mosapride is a 5HT4 agonist. Mosapride is a CYP inducer. Mosapride has a concentration-dependent inhibitory effect on Kv4.3, and its IC₅₀ value is 15.2 μM. Mosapride can be used in the study of gastrointestinal diseases.

Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole (HY-14546) and dopamine D₂/D₃ receptor partial agonist. Dehydroaripiprazole also has certain affinity for serotonin 5-HT₁A, 5-HT₂A and 5-HT₂B receptors. Dehydroaripiprazole has antipsychotic activity equivalent to Aripiprazole.

Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine₄ receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC₅₀ values of 15.2 μM. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo.

Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT_2C) receptor-selective agonist with an EC₅₀ of 8 nM.

BRL 54443 is a potent 5-HT_1E/1F receptor agonist (K_i values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors.

uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM⁴-GlyR, with an affinity of K_i of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM⁴-GlyR.

(+)-Norfenfluramine a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT_2B receptor agonist (K_i: 11.2 nM). (+)-Norfenfluramine potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca²⁺. (+)-Norfenfluramine can be used for the research of primary pulmonary hypertension and valvular heart disease.

F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with K_i of 3.4 nM.

Quipazine is a 5-HT agonist with a K_i value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC₅₀ of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research.

LP44 (hydrochloride) is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration.