5-HT Receptor Agonist

S-14506 hydrochloride is a potent 5-HT1A agonist, as well as 5-HT_2A/2C antagonist. S-14506 hydrochloride displays dopamine antagonist properties by blocking dopamine D2 receptors. S-14506 hydrochloride inhibits the in vivo binding of [3H]raclopride in striatum and olfactory bulbs. S-14506 hydrochloride has the potential for the research of anxiolytic agent.

(-)-5-HT2C agonist-3 (compound (-)-19) is a 5-HT_2C selective agonist with G_q signaling preference, with EC₅₀ values for 5-HT₂ receptors of 5-HT_2C: 103 nM; 5-HT_2B: 570 nM; 5-HT_2A: 72 nM. (-)-5-HT2C agonist-3 can be used in antipsychotic research.

Flumexadol is a selective and affinity 5-HT_2C receptor agonist with a K_i of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT_2A receptor. Flumexadol is an orally active non-narcotic analgesic.

EMD386088 is a potent and selective 5-HT6 receptor (5-HT6R) agonist with an EC₅₀ of 1.0 nM. EMD-386088 is inactive against other HT receptors except 5-HT3R (IC₅₀ of 34 nM). EMD386088 regulates the activity of ERK1/2. EMD386088 has the potential for the research of alzheimer's disease (AD) and schizophrenia.

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

Org-12962 is a potent, selective and brain-penetrant and 5-HT_2C receptor agonist with a pEC₅₀ value of 7.01. Org-12962 also exhibits high effacy for the 5-HT_2A and 5-HT_2B receptor with pEC₅₀s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.

Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with K_i values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects.

ML 10302 is a potent agonist 5-HT4 receptor with K_i of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases.

PNU-22394 hydrochloride is an agonist for 5-HT, with K_i of 6.1 and 10 nM, for 5-HT_2C and 5-HT_2A, respectively.

Aripiprazole (Standard) is the analytical standard of Aripiprazole. This product is intended for research and analytical applications. Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.

CJ033466 is a novel and selective 5-HT₄ receptor partial agonist with an EC₅₀ of 9 nM and has gastroprokinetic effect.

R(+)-8-OH-DPAT ((R)-8-Hydroxy-2-dipropylaminotetralin) hydrobromide is a potent 5-HT_1A agonist. R(+)-8-OH-DPAT potentiates SUL (HY-B1059)-induced dopamine (DA) release in the medial prefrontal cortex (mPFC).

TMU4142 is a selective 5-HT_1a agonist with high GoA activity. TMU4142 has weak Gi3 activity, can elicit rapid antidepressant like effects without triggering significant activation of dorsal raphe nucleus (DRN) 5-HT_1a R autoreceptors or serotonergic neuron firing. TMU4142 demonstrates fast-acting efficacy in mouse models of depression. TMU4142 can be used for antidepressants research.

AP521 is an agonist of human 5-HT_1A receptor with an IC₅₀ of 94 nM.

Revexepride is a highly selective 5-HT4 receptor agonist, and a potential inducer of CYP3A4 enzyme, used for the treatment of gastroesophageal reflux disease.

Ro60-0175 fumarate is a potent and selective agonist of 5-HT_2C receptor.

Parishin C (Standard) is the analytical standard of Parishin C (HY-N2125). This product is intended for research and analytical applications. 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.

Naratriptan is an orally active and selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms.

Lesopitron dihydrochloride is a full and selective 5-HT_1A receptor agonist with IC₅₀ of 125 nM in rat hippocampal membranes.

Naluzotan 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.