A selective histamine H3 receptor antagonist (Ki = 0.17 nM in rat cortical membranes); reduces inhibition of electrically induced contractions in isolated guinea pig ileum longitudinal muscle by (R)-α-methylhistamine at 0.3

Clobenpropit (hydrobromide) – 10 mg

Brand:
Cayman
CAS:
145231-35-2
Storage:
-20
UN-No:
Non-Hazardous - /

Clobenpropit is a selective histamine H3 receptor antagonist (Ki = 0.17 nM in rat cortical membranes).{19493} Clobenpropit (0.3, 0.1, and 3 nM) reduces inhibition of electrically induced contractions in isolated guinea pig ileum longitudinal muscle by the H3 receptor agonist (R)-α-methylhistamine (Item No. 25601). It does not inhibit histamine-induced contractions in isolated guinea pig ileum or tachycardia in isolated right atria at concentrations up to 1 μM, indicating a lack of functional antagonist activity at H1 and H2 receptors, respectively. Clobenpropit (1 and 3 mg/kg) decreases the duration of the tonic, clonic, and convulsive coma phases of electrically induced convulsions in mice, an effect that can be blocked by (R)-α-methylhistamine or imetit (Item No. 29517).{53229} Clobenpropit (0.1 μM) also increases GABA release and inhibits NMDA-induced neurotoxicity in primary rat cortical neurons.{16494}  

 

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SKU: 10011126 - 10 mg Category:

Description

A selective histamine H3 receptor antagonist (Ki = 0.17 nM in rat cortical membranes); reduces inhibition of electrically induced contractions in isolated guinea pig ileum longitudinal muscle by (R)-α-methylhistamine at 0.3, 0.1, and 3 nM; decreases the duration of the tonic, clonic, and convulsive coma phases of electrically induced convulsions in mice at 1 and 3 mg/kg, an effect that can be blocked by (R)-α-methylhistamine or imetit; increases GABA release and inhibits NMDA-induced neurotoxicity in primary rat cortical neurons at 0.1 μM

Formal name: N-[(4-chlorophenyl)methyl]-carbamimidothioic acid, 3-(1H-imidazol-5-yl)propyl ester, dihydrobromide

Synonyms:  VUF 9153

Molecular weight: 470.7

CAS: 145231-35-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Neuroprotection||Research Area|Neuroscience|Seizure Disorders

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