Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist

  • J Med Chem. 2006 Nov 16;49(23):6650-1. doi: 10.1021/jm060880d.
Herman D Lim  1 ,  Rogier A Smits ,  Remko A Bakker ,  Cindy M E van Dam ,  Iwan J P de Esch ,  Rob Leurs
Affiliations
  • 1. Leiden/Amsterdam Center for Drug Research, Department of Medicinal Chemistry, Vrije Universiteit Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands.
PMID: 17154494 DOI: 10.1021/jm060880d
Abstract

During an in-house database screen, we identified S-(2-guanidylethyl)-isothiourea as a high affinity agonist for the histamine H4 receptor, with a 33-fold selectivity over the histamine H3 receptor and negligible affinity for the other Histamine Receptor subtypes. This nonimidazole ligand is introduced as a useful and complementary pharmacological tool that enables further unraveling of the physiological roles of the H4 receptor.

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