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Diphenidol is an antagonist of muscarinic acetylcholine receptors (mAChRs; Kis = 0.43, 2.8, 1.1, 0.91, and 1.28 µM in CHO cell membranes expressing M1-5 receptors, respectively).1 It also inhibits Kv channels in Neuro2A cells (IC50 = 28.2 µM), as well as L-type voltage-gated calcium channels in differentiated NG 108-15 cells in a concentration-dependent manner.2 Microiontophoretic application of diphenidol inhibits rotation-induced firing of medial vestibular nucleus neurons in a cat model of vertigo.3 Diphenidol (3.2 mg/kg, i.v.) prevents apomorphine-induced emesis in dogs.4 Formulations containing diphenidol have been used in the treatment of vertigo and as antiemetics.
WARNING This product is not for human or veterinary use.
1. Diphenidol-
2. Inhibition of voltage-
3. Effects of anti-
4. Diphenidol has no actual broad antiemetic activity in dogs and ferrets. J. Pharmacol. Sci. 96(3), 301-306 (2004).