Muscarinic toxins with selectivity for muscarinic receptor subtypes: differential binding patterns in cloned and native receptors

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• 作者：Jerusalinsky ; D. ; Kornisiuk ; E. ; Harvey ; A. ; Alfaro ; P. ; Alonso ; M. ; Durá ; n ; R. ; Cerve&ntilde ; ansky ; C.
• 刊名：Life Sciences
• 出版年：1997
• 出版时间：February 21, 1997
• 年：1997
• 卷：60
• 期：13-14
• 页码：1206
• 全文大小：91.5 K

文摘

MT1, 2 (Adem et al., 1988) and 3 (Jolkkonen et al., 1994) (same as m4-toxin; Max et al., 1993) have been isolated from Dendroaspis angusticeps venom. From radioligand binding experiments with relatively selective antagonists, it was suggested that MT1 and 2 bound selectively to m1 central muscarinic receptor (Jerusalinsky et al., 1992). The K_is for MT1 and MT2, in synaptosomal membranes from cerebral cortex were range from 20-100 nM. In assays with cloned human muscarinic receptors, it was shown that both toxins have high affinity for m1 and slightly lower for m4 receptor. While MT1 and 2 have very little affinity for m5 and do not bind to m2 or m3, MT3 exhibited the highest affinity for m4 (K_i