Diphenidol hydrochloride - CAS 3254-89-5
Catalog number: 3254-89-5
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C21H28ClNO
Molecular Weight:
345.91
COA:
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Targets:
mAChR
Description:
Diphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02, respectively, used in the treatment of vomiting and vertigo.
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Purity:
>98%
Synonyms:
Diphenidol hydrochloride
MSDS:
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1.Systemic diphenidol reduces neuropathic allodynia and TNF-alpha overexpression in rats after chronic constriction injury.
Chen YW1, Tzeng JI, Liu KS, Yu SH, Hung CH, Wang JJ. Neurosci Lett. 2013 Sep 27;552:62-5. doi: 10.1016/j.neulet.2013.07.030. Epub 2013 Jul 31.
Diphenidol has been shown to block voltage-gated Na(+) channels, which are associated with specific types of pain. Here, we evaluated the effects of diphenidol on chronic constriction injury (CCI)-evoked allodynia and expression of tumor necrosis factor-α (TNF-α). A peripheral nerve injury was elicited in rats by placing four loosely constrictive ligatures around the sciatic nerve. After intraperitoneal injection of diphenidol, rats were tested for evidence of mechanical allodynia prior to surgery, and on postoperative days 3, 6, 7, 11, 13 and 14. We showed that CCI rats received diphenidol caused dose-dependent increases in mechanical withdrawal threshold. Both diphenidol 2 and 10 μmol/kg groups, but not 0.4 μmol/kg diphenidol, displayed lower TNF-α level in the sciatic nerve than the CCI group (P<0.05) on day 7 after CCI. Our results support the conclusion that systemic diphenidol produced a dose-related inhibition of mechanical allodynia following chronic constriction injury of the sciatic nerve.
2.Illicit Distribution of Prescription Drugs: Report of Inadvertent Chloroquine Toxicity and a Market Survey of Businesses Serving Ethnic Minority Populations.
Grazier MR1, Armenian P2, Vohra R3. Ann Pharmacother. 2014 May 19;48(8):1070-1076. [Epub ahead of print]
OBJECTIVE: To report a case of life-threatening cinchonism from illicit purchase of chloroquine and survey local ethnic markets to determine what medications are sold without a prescription.
3.Multiple mechanisms of ligand interaction with the human organic cation transporter, OCT2.
Harper JN1, Wright SH. Am J Physiol Renal Physiol. 2013 Jan 1;304(1):F56-67. doi: 10.1152/ajprenal.00486.2012. Epub 2012 Oct 3.
OCT2 is the entry step for organic cation (OC) secretion by renal proximal tubules. Although many drugs inhibit OCT2 activity, neither the mechanistic basis of their inhibition nor their transport status is generally known. Using representatives of several structural classes of OCT2-inhibitory ligands described recently (Kido Y, Matsson P, Giacomini KM. J Med Chem 54: 4548-4558, 2011), we determined the kinetic basis of their inhibition of 1-methyl-4-phenylpyridinium (MPP) transport into Chinese hamster ovary cells that stably expressed hOCT2. The "cluster II" inhibitors (which contain known OCT2 substrates) metformin and cimetidine interacted competitively with MPP. However, other cluster II compounds, including tetraethylammonium (TEA), diphenidol and phenyltoloxamine, were mixed-type inhibitors of MPP transport (i.e., decreasing J(max) and increasing K(t)). A cluster III (neutral steroid) representative, adrenosterone, and a cluster I (large, flexible cation) representative, carvedilol, displayed noncompetitive inhibitory profiles.
4.The expression and relaxant effect of bitter taste receptors in human bronchi.
Grassin-Delyle S1, Abrial C, Fayad-Kobeissi S, Brollo M, Faisy C, Alvarez JC, Naline E, Devillier P. Respir Res. 2013 Nov 22;14:134. doi: 10.1186/1465-9921-14-134.
BACKGROUND: Bitter-taste receptors (TAS2Rs) have recently been involved in the relaxation of mouse and guinea pig airways, and increased expression of TAS2Rs was shown in blood leucocytes from asthmatic children. We sought to identify and characterize the TAS2Rs expressed in isolated human bronchi and the subtypes involved in relaxation.
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CAS 3254-89-5 Diphenidol hydrochloride

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