Novel human histamine H 3 receptor antagonists

C Shah, L McAtee, JG Breitenbucher, D Rudolph…

Index: Shah, Chandra; McAtee, Laura; Breitenbucher, J Guy; Rudolph, Dale; Li, Xiaobing; Lovenberg, Timothy W; Mazur, Curt; Wilson, Sandy J; Carruthers, Nicholas I Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 22 p. 3309 - 3312

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Citation Number: 53

Abstract

High throughput screening, using the recombinant human H3 receptor, was used to identify novel histamine H3 receptor antagonists. Evaluation of the lead compounds ultimately afforded potent, selective, orally bioavailable compounds (eg, 38) with favorable blood– brain barrier penetration.