Synthesis, Evaluation, and Comparative Molecular Field Analysis of 1-Phenyl-3-amino-1, 2, 3, 4-tetrahydronaphthalenes as Ligands for Histamine H1 Receptors

EC Bucholtz, RL Brown, A Tropsha…

Index: Bucholtz, Ehren C.; Brown, Randal L.; Tropsha, Alexander; Booth, Raymond G.; Wyrick, Steven D. Journal of Medicinal Chemistry, 1999 , vol. 42, # 16 p. 3041 - 3054

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Citation Number: 37

Abstract

A series of 1-phenyl-3-amino-1, 2, 3, 4-tetrahydronaphthalenes (1-phenyl-3-aminotetralins, PATs) previously was found to modulate tyrosine hydroxylase activity and dopamine synthesis in rodent forebrain through interaction with a binding site labeled by [3H]-(-)-(1 R, 3 S)-trans-H2-PAT. Recently, we have discovered that PATs also bind with high affinity to the [3H] mepyramine-labeled H1 receptor in rat and guinea pig brain. Here, we report the ...