ChEBI: An imidothiocarbamic ester that consists of isothiourea bearing S-3-(imidazol-4-yl)propyl and N-4-chlorobenzyl substituents. An extremely potent histamine H3 antagonist/inverse agonist (pA
An extremely potent histamine H 3 antagonist/inverse agonist (pA 2 =9.93). Also displays partial agonist activity at H 4 receptors; induces eosinophil shape change with an EC 50 of 3 nM. Also available as part of the Histamine H 3 Receptor Tocriset™ .
Selective H3 histamine receptor antagonist that crosses the blood-brain barrier.
Clobenpropit (15 mg/kg; i.p.; once daily for 7 days) counteracts the modulatory effects of MK-801 (HY-15084B) on dopamine and histamine levels and prevents MK-801-induced hyper locomotor behaviors[1].
Clobenpropit (1, 2, 5 μmoL/kg; i.v.) causes a resuscitating effect in rats subjected to the hemorrhagic shock[2].
| Animal Model: | 150-200g, 12-week-old male wistar albino rats[1] |
| Dosage: | 15 mg/kg |
| Administration: | I.p.; once daily for 7 days |
| Result: | Exhibited a significant reduction of hyperlocomotor activities induced by a single-dose administration of MK-801 (0.2 mg/kg, i.p.), and reduced the MK-801-induced dopamine release, exhibited further increase in histamine levels in the hypothalamus. |
| Animal Model: | 205-470g, adult male Wistar rats[2] |
| Dosage: | 1, 2, 5 μmoL/kg (after 6-hydroxydopamine (50 mg/kg (SC) for 3 consecutive days) |
| Administration: | I.v. |
| Result: | Triggered a statistically significant increase of mean arterial pressure (MAP) (dose 2 μmol/kg) and heart rate (HR) (doses of 1, 2, 5 μmol/kg). |
