5-HT Receptor Agonist

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.

Bexicaserin (LP352) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related disorders (such as epilepsy).

Bretisilocin (GM-2505) is the agonist for 5-HT_2A receptor and a serotonin releaser. Bretisilocin exhibits antidepressant activity and can be used in the study of depression.

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.

Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B receptor antagonist. Tegaserod has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.

2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT₃ receptor agonist. 2-Methyl-5-HT is shown to display anti-depressive-like effects.

Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pK_is of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.

SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC₅₀) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.

Serotonin-d₄ (5-Hydroxytryptamine-d₄) hydrochloride is the deuterium labeled Serotonin (hydrochloride) (HY-B1473). Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM.

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).

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.

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.

m-CPBG (1-(3-Chlorophenyl)biguanide) hydrochloride is a selective 5-HT₃ agonist. m-CPBG hydrochloride can be used for the research of neurological disease.

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.

RU 24969 is a preferential 5-HT_1B agonist, with a K_i of 0.38 nM, but also displays appreciable affinity for the 5-HT_1A receptor (K_i=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion.

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

CP94253 hydrochloride is an orally active, brain-penetrant and selective 5-HT_1B receptor agonist with an K_i of 2 nM. CP94253 hydrochloride induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 hydrochloride can be used for the research of depression and heightened aggressive behavior.