Identification of 4-(1H-Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H3Receptor Agonist
Journal of Medicinal Chemistry2004Vol. 47(10), pp. 2414–2417
Citations Over TimeTop 24% of 2004 papers
Ruengwit Kitbunnadaj, Obbe P. Zuiderveld, B. Christophe, Saskia Hulscher, Wiro M. P. B. Menge, Edith Gelens, Erwin Snip, Remko A. Bakker, Sylvain Célanire, Michel Gillard, Patrice Talaga, Henk Timmerman, Rob Leurs
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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