Intepirdine
Intepirdine (SB742457) 是5-HT6受体拮抗剂，pKi为9.63，比对其它受体的抑制性高100倍以上。
中文名：渥曼青霉素
英文名：SB-742457; Intepirdine; GSK-742457; RVT-101
CAS 号： 607742-69-8
分子式：C₁₉H₁₉N₃O₂S
分子量：353.44
纯度：>98.0%
| Description | Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors. |
| Target | 5-HT6 Receptor |
| In Vitro | Intepirdine (SB742457), a 5-HT6 receptor antagonist, which extends into Alzheimer disease (AD) sufferers further highlights the therapeutic promise of this mechanistic approach. Alzheimer's disease is a devastating neurological condition characterized by a progressive decline in cognitive performance accompanied by behavioral and psychological syndromes, such as depression and psychosis. With the subsequent development of selective 5-HT6 receptor antagonists, preclinical studies in rodents and primates have elucidated the function of this receptor subtype in more detail. It is increasingly clear that blockade of 5-HT6 receptors leads to an improvement of cognitive performance in a wide variety of learning and memory paradigms and also results in anxiolytic and antidepressant-like activity. Intepirdine (SB742457) is generally safe and well tolerated and may be efficacious in Alzheimer disease. |
| References | [1]. Callaghan CK, Hok V, Della-Chiesa A, et al. Age-related declines in delayed non-match-to-sample performance (DNMS) are reversed by the novel 5HT6 receptor antagonist SB742457. Neuropharmacology. 2012 Oct;63(5):890-7. [2]. Codony X, Vela JM, Ramírez MJ. 5-HT(6) receptor and cognition. Curr Opin Pharmacol. 2011 Feb;11(1):94-100. [3]. Maher-Edwards G, Dixon R, Hunter J, et al. SB-742457 and donepezil in Alzheimer disease: a randomized, placebo-controlled study. Int J Geriatr Psychiatry. 2011 May;26(5):536-44. [4]. Maher-Edwards G, Zvartau-Hind M, Hunter AJ, et al. Double-blind, controlled phase II study of a 5-HT6 receptor antagonist, SB-742457, in Alzheimer's disease. Curr Alzheimer Res. 2010 Aug;7(5):374-85. [5]. Upton N, Chuang TT, Hunter AJ, Virley DJ. 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease. Neurotherapeutics. 2008 Jul;5(3):458-69. [6]. SB-742457 |
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