Identification of 4-(1H-Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H3 Receptor Agonist

Identification of 4-(1H-Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H3 Receptor Agonist

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 H3 receptor. Particularly, the 4-pyridinyl analogue of immepip (1c, immethridine) is iden...

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Veröffentlicht in:Journal of medicinal chemistry 2004-05, Vol.47 (10), p.2414-2417
Hauptverfasser: 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
Format: Artikel
Sprache:eng
Schlagworte:
Biological and medical sciences
Medical sciences
Miscellaneous
Pharmacology. Drug treatments
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Zusammenfassung: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 H3 receptor. Particularly, the 4-pyridinyl analogue of immepip (1c, immethridine) is identified as a novel potent and highly selective histamine H3 receptor agonist (pK i = 9.07, pEC50 = 9.74) with a 300-fold selectivity over the closely related H4 receptor.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm049932u