VUF 8430 dihydrobromide - CAS 100130-32-3
Category: Inhibitor
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Histamine Receptor
VUF 8430 dihydrobromide is a high affinity (pKi = 7.5) and potent histamine H4 receptor full agonist (pEC50 = 7.3). VUF 8430 also has moderate affinity for H3 receptors (pKi = 6.0) and weak partial agonist activity at H2 receptors.
Brife Description:
histamine H4 receptor agonist
VUF8430 dihydrobromide; VUF-8430 dihydrobromide; VUF 8430 dihydrobromide; 2-[(Aminoiminomethyl)amino]ethyl carbamimidothioic acid ester dihydrobromide; S-(2-guanidylethyl)-isothiourea; S,2-Guanidinoethylisothiuronium bromide hydrobromide
Canonical SMILES:
1.Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.
Lim HD;Smits RA;Bakker RA;van Dam CM;de Esch IJ;Leurs R J Med Chem. 2006 Nov 16;49(23):6650-1.
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.
2.Phenylalanine 169 in the second extracellular loop of the human histamine H4 receptor is responsible for the difference in agonist binding between human and mouse H4 receptors.
Lim HD;Jongejan A;Bakker RA;Haaksma E;de Esch IJ;Leurs R J Pharmacol Exp Ther. 2008 Oct;327(1):88-96. doi: 10.1124/jpet.108.140343. Epub 2008 Jul 17.
Using the natural variation in histamine H(4) receptor protein sequence, we tried to identify amino acids involved in the binding of H(4) receptor agonists. To this end, we constructed a variety of chimeric human-mouse H(4) receptor proteins to localize the domain responsible for the observed pharmacological differences between human and mouse H(4) receptors in the binding of H(4) receptor agonists, such as histamine, clozapine, and VUF 8430 [S-(2-guanidylethyl)-isothiourea]. After identification of a domain between the top of transmembrane domain 4 and the top of transmembrane domain 5 as being responsible for the differences in agonist affinity between human and mouse H(4)Rs, detailed site-directed mutagenesis studies were performed. These studies identified Phe(169) in the second extracellular loop as the single amino acid responsible for the differences in agonist affinity between the human and mouse H(4)Rs. Phe(169) is part of a Phe-Phe motif, which is also present in the recently crystallized beta(2)-adrenergic receptor. These results point to an important role of the second extracellular loop in the agonist binding to the H(4) receptor and provide a molecular explanation for the species difference between human and mouse H(4) receptors.
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CAS 100130-32-3 VUF 8430 dihydrobromide

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