145231-35-2
Chemical Structure
Clobenpropit dihydrobromide
- CAS No.: 145231-35-2
- Formula:C14H19Br2ClN4S
- Molecular Weight:470.65
IUPAC Name: 3-(1H-imidazol-5-yl)propyl (4-chlorobenzyl)carbamimidothioate dihydrobromide
InChIKey: JIJQPEZAVLJZBO-UHFFFAOYSA-N
SMILES: N=C(SCCCC1=CN=CN1)NCC2=CC=C(Cl)C=C2.[H]Br.[H]Br
Biological Activity: Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR[1]. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM)[2]. Clobenpropit dihydrobromide increases apoptosis[3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Clobenpropit dihydrobromide | 99.76% | Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis. | ||||||||||||||||||||
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- [1]. Esbenshade TA, et al. Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. J Pharmacol Exp Ther. 2003 Jun;305(3):887-96. [Content Brief]
- [2]. Mena-Avila E, et al. Clobenpropit, a histamine H3 receptor antagonist/inverse agonist, inhibits [3H]-dopamine uptake by human neuroblastoma SH-SY5Y cells and rat brain synaptosomes. Pharmacol Rep. 2018 Feb;70(1):146-155. [Content Brief]
- [3]. Paik WH, et al. Clobenpropit enhances anti-tumor effect of gemcitabine in pancreatic cancer. World J Gastroenterol. 2014 Jul 14;20(26):8545-57. [Content Brief]
Keywords
