Cas433282-68-9

产品名称Lecozotan HCl

别名SRA 333;SRA333;SRA-333;盐酸来考佐坦;Lecozotan HCl;Lecozotan Hydrochloride;Lecozotan hydrochloride;5-HT;5HT Receptor;5HTReceptor

计算分子量520.02

保存keep away from moisture,store at low temperature . Powder: -20°C for 3 years . In solvent: -80°C for 1 year . Shipping with blue ice.

分子式:C28H30ClN5O3
Smile:[C@H](CN(C(=O)C1=CC=C(C#N)C=C1)C2=CC=CC=N2)(C)N3CCN(C4=C5C(=CC=C4)OCCO5)CC3.Cl
DML号:MFCD11100262
纯度:99.47%
溶解度:DMSO:50 mg/mL (96.15 mM)
体内活性:Lecozotan HCl (0.3 mg/kg; s.c.) antagonized the decrease in hippocampal extracellular 5-HT induced by 8-hydroxy-2-dipropylaminotetralin (8-OH-DPAT) and had no effects alone at doses 10-fold higher. Lecozotan HCl significantly potentiated the potassium chloride-stimulated release of glutamate and acetylcholine in the dentate gyrus of the hippocampus. Chronic administration of Lecozotan HCl did not induce 5-HT(1A) receptor tolerance or desensitization in a behavioral model indicative of 5-HT(1A) receptor function.[1] In drug discrimination studies, Lecozotan HCl (0.01-1 mg/kg i.m.) did not substitute for 8-OH-DPAT and produced a dose-related blockade of the 5-HT(1A) agonist discriminative stimulus cue. In aged rhesus monkeys, Lecozotan HCl produced a significant improvement in task performance efficiency at an optimal dose (1 mg/kg p.o.). Learning deficits induced by the glutamatergic antagonist MK-801 [(-)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate] (assessed by perceptually complex and visual spatial discrimination) and by specific cholinergic lesions of the hippocampus (assessed by visual spatial discrimination) were reversed by Lecozotan HCl (2 mg/kg i.m.) in marmosets.[1]
信号通路:G 蛋白偶联受体|神经科学
靶点:5-HT Receptor