Clobenpropit dihydrobromide - CAS 145231-35-2
Category: Inhibitor
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Molecular Formula:
C14H17ClN4S.2HBr
Molecular Weight:
470.65
COA:
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Targets:
Histamine Receptor
Description:
Clobenpropit dihydrobromide is a highly potent histamine H3 antagonist/inverse agonist (pA2=9.93) that can cross blood-brain barrier. It also displays partial agonist activity at H4 receptors.
Brife Description:
histamine H3 antagonist
Purity:
≥99% by HPLC
Related CAS:
145231-45-4 (free base)
Synonyms:
N-(4-Chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea dihydrobromide
MSDS:
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InChIKey:
JIJQPEZAVLJZBO-UHFFFAOYSA-N
InChI:
InChI=1S/C14H17ClN4S.2BrH/c15-12-5-3-11(4-6-12)8-18-14(16)20-7-1-2-13-9-17-10-19-13;;/h3-6,9-10H,1-2,7-8H2,(H2,16,18)(H,17,19);2*1H
Canonical SMILES:
C1=CC(=CC=C1CN=C(N)SCCCC2=CN=CN2)Cl.Br.Br
1.Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.
Lim HD;Istyastono EP;van de Stolpe A;Romeo G;Gobbi S;Schepers M;Lahaye R;Menge WM;Zuiderveld OP;Jongejan A;Smits RA;Bakker RA;Haaksma EE;Leurs R;de Esch IJ Bioorg Med Chem. 2009 Jun 1;17(11):3987-94. doi: 10.1016/j.bmc.2009.04.007. Epub 2009 Apr 11.
Previous studies have demonstrated that clobenpropit (N-(4-chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea) binds to both the human histamine H(3) receptor (H(3)R) and H(4) receptor (H(4)R). In this paper, we describe the synthesis and pharmacological characterization of a series of clobenpropit analogs, which vary in the functional group adjacent to the isothiourea moiety in order to study structural requirements for H(3)R and H(4)R ligands. The compounds show moderate to high affinity for both the human H(3)R and H(4)R. Furthermore, the changes in the functional group attached to the isothiourea moiety modulate the intrinsic activity of the ligands at the H(4)R, ranging from neutral antagonism to full agonism. QSAR models have been generated in order to explain the H(3)R and H(4)R affinities.
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CAS 145231-35-2 Clobenpropit dihydrobromide

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