Structure-affinity profile of 8-hydroxycarbostyril-based agonists that dissociate slowly from the β2-adrenoceptor

MD Deyrup, ST Nowicki, NGJ Richards…

Index: Deyrup; Nowicki; Richards; Otero; Harrison; Baker Naunyn-Schmiedeberg's Archives of Pharmacology, 1999 , vol. 359, # 3 p. 168 - 177

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Citation Number: 21

Abstract

Abstract Several carbostyril-based β-agonists have been shown to bind tightly to and slowly dissociate from the β 2-adrenoceptor (β 2 AR). In the present study, the structural features of 8-hydroxy-5-[2-[(1-phenyl-2-methylprop-2-yl) amino]-1-hydroxyethyl]-carbostyril (11a) which contribute to its binding properties at the β 2 AR were investigated using a series of synthesized analogs. The k off, estimated by the rate of cAMP decline in DDT 1 MF-2 (DDT ...