2928181-97-7

Diphenidol-d10 is intended for use as an internal standard for the quantification of diphenidol (Item No. 18674) by GC- or LC-MS. 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] LUCILLA VAROLI . Diphenidol-related diamines as novel muscarinic M4 receptor antagonists[J]. Bioorganic & Medicinal Chemistry Letters, 2008, 18 9: Pages 2972-2976. DOI: 10.1016/j.bmcl.2008.03.061
[2] YUK-MAN LEUNG . Inhibition of voltage-gated K+ channels and Ca2+ channels by diphenidol[J]. Pharmacological Reports, 2012, 64 3: Pages 739-744. DOI: 10.1016/s1734-1140(12)70869-1
[3] ATSUHIKO KAWABATA . Effects of Anti-Vertigo Drugs on Medial Vestibular Nucleus Neurons Activated by Horizontal Rotation[J]. Japanese journal of pharmacology, 1991, 55 1: Pages 101-106. DOI: 10.1016/s0021-5198(19)39982-2
[4] HIROE NAKAYAMA . Diphenidol Has No Actual Broad Antiemetic Activity in Dogs and Ferrets[J]. Journal of pharmacological sciences, 2004, 96 3: Pages 301-306. DOI: 10.1254/jphs.fpj04035x