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Identification of 4-(1H-Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H Receptor Agonist

Journal of Medicinal Chemistry, ISSN: 0022-2623, Vol: 47, Issue: 10, Page: 2414-2417
2004
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Article Description

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 receptor. Particularly, the 4-pyridinyl analogue of immepip (1c, immethridine) is identified as a novel potent and highly selective histamine H receptor agonist (pK = 9.07, pEC = 9.74) with a 300-fold selectivity over the closely related H receptor.

Bibliographic Details

Kitbunnadaj, Ruengwit; Zuiderveld, Obbe P; Christophe, Bernard; Hulscher, Saskia; Menge, Wiro M P B; Gelens, Edith; Snip, Erwin; Bakker, Remko A; Celanire, Sylvain; Gillard, Michel; Talaga, Patrice; Timmerman, Henk; Leurs, Rob

American Chemical Society (ACS)

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics

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