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Lecozotan HCl (SRA-333) 是一种强效且具有选择性的 5-HT 拮抗剂。Lecozotan HCl能明显增强氯化钾刺激海马齿状回谷氨酸和乙酰胆碱的释放并具有增强认知能力的特性。在表明 5-HT(1A) 受体功能的行为模型中,长期服用Lecozotan HCl不会诱发 5-HT(1A) 受体耐受或脱敏。
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Lecozotan HCl (SRA-333) 是一种强效且具有选择性的 5-HT 拮抗剂。Lecozotan HCl能明显增强氯化钾刺激海马齿状回谷氨酸和乙酰胆碱的释放并具有增强认知能力的特性。在表明 5-HT(1A) 受体功能的行为模型中,长期服用Lecozotan HCl不会诱发 5-HT(1A) 受体耐受或脱敏。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,130 | 现货 | |
5 mg | ¥ 2,760 | 现货 | |
10 mg | ¥ 3,970 | 现货 | |
25 mg | ¥ 6,560 | 现货 | |
50 mg | ¥ 8,930 | 现货 | |
100 mg | ¥ 11,800 | 现货 | |
500 mg | ¥ 23,900 | 6-8周 |
产品描述 | Lecozotan HCl (SRA-333) is a potent and selective 5-HT antagonist that significantly enhances KCl-stimulated glutamate and acetylcholine release from the hippocampal dentate gyrus and has cognitive enhancing properties. Chronic administration of Lecozotan HCl did not induce 5-HT(1A) receptor tolerance or desensitization in a behavioral model demonstrating 5-HT(1A) receptor function. |
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] |
别名 | 盐酸来考佐坦, SRA-333, SRA333, SRA 333, Lecozotan hydrochloride |
分子量 | 520.02 |
分子式 | C28H30ClN5O3 |
CAS No. | 433282-68-9 |
Smiles | [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 |
密度 | 1.31g/cm3 |
存储 | 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. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (96.15 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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