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Literature DB >> 17154494

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

Herman D Lim¹, Rogier A Smits, Remko A Bakker, Cindy M E van Dam, Iwan J P de Esch, Rob Leurs.

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.

Entities: Chemical Gene

Mesh：

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Year: 2006 PMID： 17154494 DOI： 10.1021/jm060880d

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

16 in total

Review 1. Molecular and biochemical pharmacology of the histamine H4 receptor.

Authors: Rob Leurs; Paul L Chazot; Fiona C Shenton; Herman D Lim; Iwan J P de Esch
Journal: Br J Pharmacol Date: 2009-05 Impact factor: 8.739

2. The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

Authors: Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal: Br J Pharmacol Date: 2013-12 Impact factor: 8.739

3. Molecular determinants for the high constitutive activity of the human histamine H4 receptor: functional studies on orthologues and mutants.

Authors: D Wifling; K Löffel; U Nordemann; A Strasser; G Bernhardt; S Dove; R Seifert; A Buschauer
Journal: Br J Pharmacol Date: 2014-09-05 Impact factor: 8.739

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

Review 1. Molecular and biochemical pharmacology of the histamine H4 receptor.

2. The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

3. Molecular determinants for the high constitutive activity of the human histamine H4 receptor: functional studies on orthologues and mutants.

Review 4. International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.

Review 5. Molecular and cellular analysis of human histamine receptor subtypes.

6. Differential effects of functionally different histamine H₄ receptor ligands on acute irritant dermatitis in mice.

7. Postsynaptic mechanisms underlying the excitatory action of histamine on medial vestibular nucleus neurons in rats.

8. Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430.

9. Profiling of histamine H4 receptor agonists in native human monocytes.

10. Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells.