SEP-363856 (hydrochloride)

SEP-363856 is an agonist of trace amine-associated receptor 1 (TAAR1). It increases intracellular cAMP levels in cells expressing TAAR1 (EC50 = 0.14 µM). It is also an agonist of the serotonin (5-HT) receptor subtypes 5-HT1D and 5-HT1A, decreasing cAMP levels in cells expressing these receptors (EC50s = 0.262 and 2.3 µM, respectively). SEP-363856 is selective for these receptors over the dopamine D2L receptor (EC50s = 10.44 and 8.02 µM in cAMP and arrestin recruitment assays, respectively), as well as alpha2A- and alpha2B-adrenergic, and 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT7 receptors (EC50s = 6.7->10 µM in functional assays). It reduces hyperactivity induced by phencyclidine (PCP) in mice when administered at 0.3, 1, and 3 mg/kg and reverses PCP-induced impairments in social interaction in rats. SEP-363856 (3, 10, and 30 mg/kg) increases prepulse inhibition of the acoustic startle response in mice. It also decreases the time spent immobile in the forced swim test in mice, indicating antidepressant-like activity.Formal Name: 4,7-dihydro-N-methyl-5H-thieno[2,3-c]pyran-7-methanamine, monohydrochloride. CAS Number: 1310422-41-3. Synonyms: SEP-856. Molecular Formula: C9H13NOS . HCl. Formula Weight: 219.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 2 mg/ml, Ethanol: 0.2 mg/ml, PBS (pH 7.2): 1 mg/ml. SMILES: CNC[C@H]1C2=C(CCO1)C=CS2.Cl. InChi Code: InChI=1S/C9H13NOS.ClH/c1-10-6-8-9-7(2-4-11-8)3-5-12-9,/h3,5,8,10H,2,4,6H2,1H3,1H/t8-,/m0./s1. InChi Key: JRDQGVVFSHRVTL-QRPNPIFTSA-N.