CM699 (hydrochloride)

A dual sigma receptor antagonist (Kis = 0.0141 and 0.00231 µM for the sigma1 and sigma2 receptors, respectively) and DAT inhibitor (Ki = 0.311 µM), selective for the sigma1 and sigma2 receptors and DAT over SERT (Ki = 2.83 µM) but also binds to NET (Ki = 0.232 µM), inhibits dopamine uptake in rat striatal synaptosomes (IC50 = 6.01 µM) and induces sigma1 receptor multimerization, indicating antagonist activity, in HEK293 cells expressing the human receptor at 20 µM, decreases self-administration of cocaine in rats. Formulation: A neat solid. InChI: InChI=1S/C24H29N3O2.ClH/c1-25-21-10-4-5-11-22(21)27(23(25)28)15-7-6-14-26-16-12-24(13-17-26)20-9-3-2-8-19(20)18-29-24,/h2-5,8-11H,6-7,12-18H2,1H3,1H. InChIKey: IQIQXQIYPCEHPA-UHFFFAOYSA-N. SMILES: CN1C2=C(C=CC=C2)N(C1=O)CCCCN3CCC4(CC3)C5=C(CO4)C=CC=C5.Cl