5-HT₁ Receptor Agonist

SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT₂ and 5-HT_1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM.

Dihydroergotamine mesylate is a blood-brain barrier-permeable semi-synthetic ergot alkaloid, acting as a full agonist of 5-HT1B/1D receptors (K_i values of 0.3 nM and 2.5 nM, respectively; functional IC₅₀ values of 2 nM and 2.2 nM, respectively). Dihydroergotamine mesylate inhibits Forskolin (HY-15371)-stimulated cAMP accumulation, possesses α-adrenergic receptor antagonistic activity and weak dopaminergic agonistic activity. It mediates intracranial cerebrovascular contraction, inhibits the release of neuropeptides such as CGRP/substance P, and suppresses neurogenic inflammation by activating 5-HT1B/1D receptors in the trigeminovascular system. Dihydroergotamine mesylate binds to the catalytic site of Trypanosoma cruzi trypanothione reductase and exhibits trypanocidal activity in vitro. Dihydroergotamine mesylate can be used in studies related to migraine and trypanosome infections.

Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.

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.

8-OH-DPAT is a potent, brain-penetrant and selective 5-HT agonist, with a pIC₅₀ of 8.19 for 5-HT1A and a K_i of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC₅₀, 5.42), 5-HT (pIC₅₀ <5).

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.

Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT₁A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.

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 (ICI204636) is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.

Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT_1A receptor partial agonist.

Rotigotine is a potent dopamine receptor agonist with K_i values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research.

Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC₅₀s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT_1D, 5-HT_1B and 5-HT_1F receptors, respectively. Sumatriptan can be used for migraine headache research.

Rotigotine Hydrochloride (N-0923 Hydrochloride) 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_i of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

Buspirone hydrochloride is a 5-HT1A receptor agonist. Buspirone hydrochloride can be used for anxiety and depression research.

8-OH-DPAT (8-Hydroxy-DPAT) hydrobromide is a potent, brain-penetrant and selective 5-HT_1A agonist with a pIC₅₀ of 8.19. 8-OH-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT₁ binding site.

LP-211 is a selective and blood brain barrier penetrant 5-HT₇ receptor agonist, with a K_i of 0.58 nM, with high selectivity over 5-HT_1A receptor (K_i, 188 nM) and D₂ receptor (K_i, 142 nM).

BMY 7378 is a selective antagonist of α_1D-adrenoceptor (α_1D-AR). BMY 7378 binds to membranes expressing the cloned rat α_1D-AR with a >100-fold higher affinity (K_i=2 nM) than binding to either the cloned rat α_1A-AR (K_i=800 nM) or the hamster α_1B-AR (K_i=600 nM). BMY 7378 is a 5-HT_1A receptor partial agonist.

RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pK_i of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research.

Rizatriptan benzoate is the agonist for 5-HT_1B and 5-HT_1D. Rizatriptan benzoate has a peripheral vasoconstrictive effect, penetrates the intact blood-brain barrier, and inhibits pain neurotransmission in the central nervous system.

Sumatriptan succinate (GR 43175) is an orally active 5-HT1 receptor agonist with IC₅₀s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT_1D, 5-HT_1B and 5-HT_1F receptors, respectively. Sumatriptan succinate can be used for migraine headache research.