5-HT₃ Receptor 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.

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

Amanozine (Compound 15) is a 5-HT₃ serotonin receptor agonist. Amanozine is promising for research of nervous system disorders.

PSN09 is a blood-brain barrier-permeable agonist of PSAM⁴-GlyR and PSAM⁴-5-HT₃ receptors with high affinity. 18F-labeled PSN09 serves as a radiotracer for PET imaging in non-human primates.

GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a α4β2 (K_i=20 nM for humanα4β2) and 5-HT3A receptor (IC₅₀=3.1 μM) antagonist. GTS-21 can be used in age-associated memory impairment (AAMI) and Alzheimer's disease research.

A-582941 is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with K_i values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 exhibits agonistic activity at 5-HT3 receptors, with a K_i of 150 nM. A-582941 triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 is applicable for the research of Alzheimer's disease and schizophrenia.

CSP-2503 is a potent and selective 5-HT_1A receptor agonist , with an EC₅₀ of 0.15 μM and a K_i of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (K_i > 1000 nM), 5-HT₄ receptors, and benzodiazepine receptors. CSP-2503 inhibits cAMP increase in vitro and exhibits anxiolytic activity in vivo. CSP-2503 can be used for the research of anxiety-related disorders.

RS-56812 is a partial agonist of the 5-HT₃ receptor. RS-56812 significantly enhances the propulsive peristalsis of the colon. RS-56812 indirectly enhances cholinergic neurotransmission and improves the working memory performance of non-human primates. RS-56812 is used in research on diarrhea/colon peristalsis and cognitive disorders (such as Alzheimer's disease).