Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.

Abstract

In this study, the piperidine ring of immepip and its analogues was replaced by a rigid heterocyclic pyridine ring. Many compounds in the series exhibit high affinity and agonist activity at the human histamine H(3) receptor. Particularly, the 4-pyridinyl analogue of immepip (1c, immethridine) is identified as a novel potent and highly selective histamine H(3) receptor agonist (pK(i) = 9.07, pEC(50) = 9.74) with a 300-fold selectivity over the closely related H(4) receptor.

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@article{Kitbunnadaj2004IdentificationO4, title={Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.}, author={Ruengwit Kitbunnadaj and Obbe P. Zuiderveld and Bernard Christophe and Saskia T M Hulscher and Wiro M. P. B. Menge and Edith Gelens and Erwin Snip and Remko A. Bakker and Sylvain C{\'e}lanire and Michel R Gillard and Patrice E Talaga and Henk Timmerman and Rob Leurs}, journal={Journal of medicinal chemistry}, year={2004}, volume={47 10}, pages={2414-7} }