1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  2. mAChR Sodium Channel
  3. Diphenidol

Diphenidol is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol can be used in the study of antivertigo and antinausea.

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Diphenidol

Diphenidol Chemical Structure

CAS No. : 972-02-1

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Description

Diphenidol is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol can be used in the study of antivertigo and antinausea[1][2][3][4][5].

IC50 & Target

mAChR1

 

mAChR2

 

mAChR3

 

mAChR4

 

In Vitro

Diphenidol inhibits sodium currents and produces spinal anesthesia, and at -70 and -100 mV holding potentials, N2A cells IC50 were 0.77 and 62.6 μM, respectively [3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Diphenidol (2, 10 μmoL/kg, intraperitoneal injection) is used to reduce neuropathic pain and TNF-α overexpression in rats after chronic systolic injury[4].
Diphenidol (30 mg/kg, injected intravenously) has an inhibitory effect on exercise and morphine-induced vomiting in pica rats[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Chronic constriction injury (CCI) rat model[4]
Dosage: 2, 10 μmoL/kg
Administration: i.p., berore surgery, and on postoperative days 3, 6, 7, 11, 13 and 14.
Result: Increased mechanical withdrawal threshold in a dose-dependent manner and decreased the TNF-α level.
Molecular Weight

309.45

Formula

C21H27NO

CAS No.
SMILES

OC(C1=CC=CC=C1)(C2=CC=CC=C2)CCCN3CCCCC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Diphenidol
Cat. No.:
HY-A0270
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