Ultrapotent PSEM (uPSEM) agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki = 0.7 nM for PSAM4-GlyR and <10 nM for PSAM4-5HT3). Exhibits >10,000-fold agonist selectivity for PSAM4-GlyR over alpha7-GlyR, alpha7-5HT3, and 5HT3-R, and 230-fold selectivity over alpha4beta2 nAChR. Also weak partial agonist (~10 %) at alpha4beta2 nAChR. Retains the potency of varenicline for PSAM4-GlyR with enhanced chemogenetic selectivity. Does not act as a substrate for P-glycoprotein pumps. Silences neurons in vivo. Brain-penetrant.
Target-Kategorie:
Others
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