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

Journal of Medicinal Chemistry

Volumn 49, Issue 23, 2006, Pages 6650-6651

  Lim, Herman D ^a   Smits, Rogier A ^a   Bakker, Remko A ^a   Van Dam, Cindy M E ^a   De Esch, Iwan J P ^a   Leurs, Rob ^a  

^a VU UNIVERSITY AMSTERDAM   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

DIMAPRIT; HISTAMINE AGONIST; HISTAMINE H4 RECEPTOR; HISTAMINE H4 RECEPTOR AGONIST; JNJ 7777120; LIGAND; RECEPTOR SUBTYPE; S (2 GUANIDYLETHYL)ISOTHIOUREA; UNCLASSIFIED DRUG; VUF 6002;

ANIMAL CELL; ARTICLE; BINDING COMPETITION; CHO CELL; CONCENTRATION RESPONSE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; NONHUMAN; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION;

BETA-GALACTOSIDASE; CELL LINE, TUMOR; GUANIDINES; HISTAMINE AGONISTS; HUMANS; RADIOLIGAND ASSAY; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, HISTAMINE; STRUCTURE-ACTIVITY RELATIONSHIP; THIOUREA;

EID: 33750993771     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm060880d     Document Type: Article

References (14)

1. Hough, L. B. Genomics meets histamine receptors: new subtypes, new receptors. Mol. Pharmacol. 2001, 59, 415-419.
2. 4 receptor on human eosinophils-role in eosinophil chemotaxis. J. Recept. Signal Transduction Res. 2002, 22, 431-448.
3. 4 receptor mediates chemotaxis and calcium mobilization of mast cells. J. Pharmacol. Exp. Ther. 2003, 305, 1212-1221.
4. + T cells. J. Pharmacol. Exp. Ther. 2002, 303, 300-307.
5. 4 production and mast cell-dependent neutrophil recruitment induced by zymosan in vivo. J. Pharmacol. Exp. Ther. 2003, 307, 1072-1078.
6. 4 receptor as a new therapeutic target for inflammation. Trends Pharmacol. Sci. 2005, 26, 462-469.
7. 4 receptor antagonist with anti-inflammatory properties. J. Pharmacol. Exp. Ther. 2004, 309, 404-413.
8. 4 receptor antagonists. Bioorg. Med. Chem. Lett. 2004, 14, 5251-5256.
9. 4-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5-[1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine. J. Med. Chem. 2003, 46, 3162-3165.
10. 4 receptor agonist. J. Pharmacol. Exp. Ther. 2005, 314, 1310-1321.
11. 4) expressed in bone marrow. Mol. Pharmacol. 2001, 59, 420-426.
12. 2-activity. Agents Actions 1986, 18, 137-140.
13. 2-receptor. Dissertation Vrije Universiteit Amsterdam 1987, 125-136.
14. Shapira, R.; Doherty, D. G.; Burnett, W. T., Jr. Chemical protection against ionizing radiation. III. Mercaptoalkylguanidines and related isothiuronium compounds with protective activity. Radiat. Res. 1957, 7, 22-34.