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

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

  • J Med Chem. 2004 May 6;47(10):2414-7. doi: 10.1021/jm049932u.
Ruengwit Kitbunnadaj 1,  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
Affiliations

Affiliation

  • 1 Leiden/Amsterdam Center of Drug Research (LACDR), Division of Medicinal Chemistry, Faculty of Sciences, Vrije Universiteit Amsterdam, The Netherlands.
PMID: 15115383 DOI: 10.1021/jm049932u
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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