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Clobenpropit is a selective histamine H3 receptor antagonist (Ki = 0.17 nM in rat cortical membranes).[1] 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. 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.[2] Clobenpropit (0.1 μM) also increases GABA release and inhibits NMDA-induced neurotoxicity in primary rat cortical neurons.[3]

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