Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.
Ruengwit Kitbunnadaj, Obbe P Zuiderveld, Bernard Christophe, Saskia Hulscher, Wiro M P B Menge, Edith Gelens, Erwin Snip, Remko A Bakker, Sylvain Celanire, Michel Gillard, Patrice Talaga, Henk Timmerman, Rob Leurs
文献索引：J. Med. Chem. 47 , 2414-2417, (2004)
全文：HTML全文
摘要
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.