… Studies of 7-Substituted-1, 2, 3, 4-tetrahydroisoquinolines and Their Relative Affinities toward Phenylethanolamine N-Methyltransferase and the α2-Adrenoceptor, 1

GL Grunewald, VH Dahanukar, RK Jalluri…

Index: Grunewald, Gary L.; Dahanukar, Vilas H.; Jalluri, Ravi K.; Criscione, Kevin R. Journal of Medicinal Chemistry, 1999 , vol. 42, # 1 p. 118 - 134

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Citation Number: 30

Abstract

7-Substituted-1, 2, 3, 4-tetrahydroisoquinolines (7-substituted-THIQs) are potent inhibitors of phenylethanolamine N-methyltransferase (PNMT, EC 2.1. 1.28), the enzyme involved in the biosynthesis of epinephrine. Unfortunately, most of these compounds also exhibit strong affinity for the α2-adrenoceptor. To design a selective (PNMT vs α2-adrenoceptor affinity) inhibitor of PNMT, the steric and electrostatic factors responsible for PNMT inhibitory ...