Difenidol

Diphenidol is an orally active antiemetic. Diphenidol reduces abnormal neuropathic pain and TNF-α overexpression in rats following chronic compression injury. Diphenidol also has local anaesthetic activity and inhibits sodium currents. Diphenidol can be used in studies of meniere′s disease, anti-vertigo, antiemetic and analgesia[1][2].

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

Diphenidol (0.1-100 µM) blocks Na+ currents with an IC50 of 0.77 µM and a Hill coefficient of 1.15 in N2A cells[1].

Diphenidol (0.77 mg/rat; intrathecal injection; single) blocks motor function, proprioception, and nociception in rats[1]. Diphenidol (0.62, 3.09 mg/kg; i.p.; single daily for 7 days) effectively reverses or completely blocks CCI-evoked mechanical allodynia in rats[2]. Animal Model: Male SpragueeDawley rats (275-325 g)[1]. Dosage: 0.77 mg/rat (2.50 µmol/rat) Administration: Intrathecal injection; single. Result: Caused 100% of blockades in motor function, proprioception, and nociception with durations of action of about 51, 77, and 123 min, respectively. Animal Model: Male adult Sprague-Dawley rats (200-250 g; CCI rat model)[2]. Dosage: 0.62, 3.09 mg/kg (2, 10 µmol/kg) Administration: Intraperitoneal injection; single daily for 7 days. Result: Blocked the CCI-induced low mechanical withdrawal threshold at 1 h after administration. Reduced the level of TNF-α on day 7 and alleviated neuropathic tactile allodynia following CCI in rats.

DATA ITEMS CITED :

5

MOLECULAR FORMULA :

C21-H27-N-O

MOLECULAR WEIGHT :

309.49

WISWESSER LINE NOTATION :

T6NTJ A3XQR&R

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

815 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

PHMCAA Pharmacologist. (American Soc. for Pharmacology and Experimental Therapeutics, 9650 Rockville Pike, Bethesda, MD 20014) V.1- 1959- Volume(issue)/page/year: 5,265,1963

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

304 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

450 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

PHMCAA Pharmacologist. (American Soc. for Pharmacology and Experimental Therapeutics, 9650 Rockville Pike, Bethesda, MD 20014) V.1- 1959- Volume(issue)/page/year: 5,265,1963

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

103 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

LACHDL Liebigs Annalen der Chemie. (Verlag Chemie International, Inc., VCH Pub., Inc., 303 N.W. 12th Ave., Deerfield Beach, FL 33441) No. 1- 1979- Volume(issue)/page/year: (10),1554,1979

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

32 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

MPHEAE Medicina et Pharmacologia Experimentalis. (Basel, Switzerland) V.12-17, 1965-67. For publisher information, see PHMGBN. Volume(issue)/page/year: 13,325,1965