NAS-181

NAS-181 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT1B (Ki = 47 nM for the rat receptor). It is selective for 5-HT1B over 5-HT1A, 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 (Kis = >3,000 nM for all for the rat receptors). NAS-181 (100 or 1,000 nM) potentiates potassium-stimulated 5-HT release in isolated and preloaded rat occipital cortical slices. It increases extracellular levels of acetylcholine (ACh), but not glutamate or GABA, in the frontal cortex and ventral hippocampus of non-anesthetized rats when administered at doses of 1, 5, or 10 mg/kg. NAS-181 (3 mg/kg) induces wet-dog shakes in rats, an effect that can be prevented by the tryptophan hydroxylase inhibitor p-chloro phenylalanine (Cay-26168). It increases the length of freezing time induced by contextual fear conditioning in mice.Formal Name: (2R)-2-[[[3-(4-morpholinylmethyl)-2H-1-benzopyran-8-yl]oxy]methyl]-morpholine, bimethanesulfonate. CAS Number: 1217474-40-2. Molecular Formula: C19H26N2O4 . 2CH3SO3H. Formula Weight: 538.6. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble, DMSO: Soluble, Methanol: Soluble, Water: Soluble. SMILES: CS(=O)(O)=O.CS(=O)(O)=O.N1(CC2=CC3=CC=CC(OC[C@@H]4OCCNC4)=C3OC2)CCOCC1. InChi Code: InChI=1S/C19H26N2O4.2CH4O3S/c1-2-16-10-15(12-21-5-8-22-9-6-21)13-25-19(16)18(3-1)24-14-17-11-20-4-7-23-17,2*1-5(2,3)4/h1-3,10,17,20H,4-9,11-14H2,2*1H3,(H,2,3,4)/t17-,,/m1../s1. InChi Key: WMRMIRRDPBKNMY-ZEECNFPPSA-N.