Effects of a 3-Alkyl-, 4-Hydroxy-and/or 8-Aromatic-substituent on the Phenylethanolamine N-Methyltransferase Inhibitor Potency and α 2-Adrenoceptor Affinity of 2, 3, 4 …

GL Grunewald, VH Dahanukar, KR Criscione

Index: Grunewald, Gary L.; Dahanukar, Vilas H.; Criscione, Kevin R. Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 8 p. 1957 - 1965

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Citation Number: 16

Abstract

2, 3, 4, 5-Tetrahydro-1H-2-benzazepine (THBA; 1) is nearly 100-fold more selective an inhibitor of phenylethanolamine N-methyltransferase (PNMT, EC 2.1. 1.28) versus the α2- adrenoceptor than is 1, 2, 3, 4-tetrahydroisoquinoline (THIQ; 2)(1: PNMT Ki= 3.3 μM, α2- adrenoceptor Ki= 11μM, selectivity [α2Ki/PNMT Ki]= 3.3; 2: PNMT Ki= 9.7 μM, α2Ki= 0.35 μM, selectivity= 0.036;). Since the PNMT inhibitory activity and selectivity of THIQ were ...