MDL 73005EF: partial agonist at the 5-HT1A receptor negatively linked to adenylate cyclase.
MDL 73005EF: partial agonist at the 5-HT1A receptor negatively linked to adenylate cyclase.
复制标题
MDL 73005EF：与腺苷酸环化酶负相关的 5-HT1A 受体的部分激动剂。
DOI：
10.1016/0014-2999(89)90518-9
复制
发表时间：
1989
影响因子：
5
通讯作者：
Martin,AR
中科院分区：
文献类型：
--
作者：
Cornfield,LJ;Nelson,DL;Taylor,EW;Martin,AR
MDL 73005EF 最近被描述为一种有效的、高选择性的 5-HT1 配体。尽管建议主要充当拮抗剂（M. Hibert、A.K. Mir、G. Maghioros、P. Moser、D.N. Middlemiss、M.D. Trickleband 和 J.R. Fozard，1988，MDL 73005EF 的药理学特性：5-HT1A 受体的有效且选择性配体，Br. J. Pharmacol. 93，2P），但我们已经证明MDL 73005EF 还可以作为 5-HT1A 受体的高效部分激动剂，因为它能够抑制大鼠海马膜中毛喉素刺激的腺苷酸环化酶。与两种结构相关的 5-HT1Apartial 激动剂相比，FSC 测定中 MDL 73005EF 的效力排序与通过放射性配体结合计算的亲和力相当。
MDL 73005EF has been recently described as a potent, highly selective 5-HT1Aligand. Although proposed to act predominantly as an antagonist (M. Hibert, A.K. Mir, G. Maghioros, P. Moser, D.N. Middlemiss, M.D. Trickleband and J.R. Fozard, 1988, The pharmacological properties of MDL 73005EF: a potent and selective ligand at 5-HT1Areceptors, Br. J. Pharmacol. 93, 2P), we have demonstrated that MDL 73005EF also acts as a highly efficacious partial agonist at the 5-HT1Areceptor, based on its ability to inhibit forskolin-stimulated adenylate cyclase in rat hippocampal membranes. Compared with two structurally related 5-HT1Apartial agonists, the rank order of potency of MDL 73005EF in the FSC assay was comparable to affinity calculated by radioligand binding.