Cornfield L J, Nelson D L, Taylor E W, Martin A R
Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson 85721.
Eur J Pharmacol. 1989 Dec 7;173(2-3):189-92. doi: 10.1016/0014-2999(89)90518-9.
MDL 73005EF has been recently described as a potent, highly selective 5-HT1A ligand. 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 ligant at 5-HT1A receptors, Br. J. Pharmacol. 93, 2P), we have demonstrated that MDL 73005EF also acts as a highly efficacious partial agonist at the 5HT1A receptor, based on its ability to inhibit forskolin-stimulated adenylate cyclase in rat hippocampal membranes. Compared with two structurally related 5-HT1A partial agonists, the rank order of potency of MDL 73005EF in the FSC assay was comparable to affinity calculated by radioligand binding.
MDL 73005EF最近被描述为一种强效、高选择性的5-羟色胺1A（5-HT1A）配体。尽管它主要被认为是一种拮抗剂（M. 希伯特、A.K. 米尔、G. 马吉奥罗斯、P. 莫泽、D.N. 米德米斯、M.D. 特里克尔班德和J.R. 福扎德，1988年，《MDL 73005EF的药理学特性：一种强效且选择性的5-HT1A受体配体》，《英国药理学杂志》93卷，2P），但我们已经证明，基于MDL 73005EF抑制大鼠海马膜中福斯高林刺激的腺苷酸环化酶的能力，它在5-HT1A受体上也作为一种高效的部分激动剂起作用。与两种结构相关的5-HT1A部分激动剂相比，MDL 73005EF在福斯高林刺激的腺苷酸环化酶（FSC）测定中的效价顺序与通过放射性配体结合计算的亲和力相当。
