NAN-190

NAN-190 is a mixed antagonist and partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A. It inhibits radioligand binding to 5-HT1A sites in rat hippocampal membranes (Ki = 2 nM). NAN-190 decreases 5-carboxamidotryptamine-mediated inhibition of forskolin-induced adenylyl cyclase activity in guinea pig hippocampal membranes in a concentration-dependent manner, indicating partial agonist activity. NAN-190 also antagonizes alpha1-adrenergic receptors (alpha1-ARs, pA2s = 9.47, 9.02, and 9.99 in isolated rat tail artery, rabbit aorta, and rat aorta, respectively). In vivo, NAN-190 (1-300 µg/kg) decreases blood pressure, without modifying heart rate, in anesthetized rats. It inhibits phenylephrine-induced pressor responses in pithed rats. NAN-190 (5 mg/kg, i.p.) potentiates the circadian response to light in dark-adapted and entrained hamsters.Formal Name: 2-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-1H-isoindole-1,3(2H)-dione, monohydrobromide. CAS Number: 115338-32-4. Molecular Formula: C23H27N3O3 . HBr. Formula Weight: 474.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 214, 219, 233, 241 nm. SMILES: O=C1N(CCCCN2CCN(C3=CC=CC=C3OC)CC2)C(C4=CC=CC=C41)=O.Br. InChi Code: InChI=1S/C23H27N3O3.BrH/c1-29-21-11-5-4-10-20(21)25-16-14-24(15-17-25)12-6-7-13-26-22(27)18-8-2-3-9-19(18)23(26)28,/h2-5,8-11H,6-7,12-17H2,1H3,1H. InChi Key: AXRUEPFPTQYHQD-UHFFFAOYSA-N.