Difenidol

Modify Date: 2024-01-08 14:27:36

Difenidol structure	Common Name	Difenidol
	CAS Number	972-02-1	Molecular Weight	309.44500
	Density	1.066 g/cm3	Boiling Point	473.3ºC at 760 mmHg
	Molecular Formula	C₂₁H₂₇NO	Melting Point	105ºC
	MSDS	N/A	Flash Point	233.5ºC

Use of 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].

Name	diphenidol
Synonym	More Synonyms

Description	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].
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Neurological Disease
In Vitro	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].
In Vivo	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.

Density	1.066 g/cm3
Boiling Point	473.3ºC at 760 mmHg
Melting Point	105ºC
Molecular Formula	C₂₁H₂₇NO
Molecular Weight	309.44500
Flash Point	233.5ºC
Exact Mass	309.20900
PSA	23.47000
LogP	4.12650
Index of Refraction	1.5614 (estimate)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM4970000

CHEMICAL NAME :: 1-Piperidinebutanol, alpha,alpha-diphenyl-

CAS REGISTRY NUMBER :: 972-02-1

BEILSTEIN REFERENCE NO. :: 0265884

LAST UPDATED :: 199612

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

HS Code	2933399090

Piperidine

CAS#:110-89-4

carbon monoxide

CAS#:201230-82-2

α-ethenyl-α-phe...

CAS#:3923-51-1

~10%

Difenidol

CAS#:972-02-1

Literature: Schmidt, Andreas; Marchetti, Mauro; Eilbracht, Peter Tetrahedron, 2004 , vol. 60, # 50 p. 11487 - 11492

Benzophenone

CAS#:119-61-9

Difenidol

CAS#:972-02-1

Literature: Helvetica Chimica Acta, , vol. 24, p. 209 E, 220 E Journal of the American Chemical Society, , vol. 74, p. 4085

Piperidine

CAS#:110-89-4

4-hydroxy-4,4-d...

CAS#:63645-18-1

Difenidol

CAS#:972-02-1

Literature: Journal of Organometallic Chemistry, , vol. 332, p. 9 - 18

Piperidine

CAS#:110-89-4

Difenidol

CAS#:972-02-1

Literature: GB683950 , ;

Precursor 5
CAS#:110-89-4 Piperidine CAS#:201230-82-2 carbon monoxide CAS#:3923-51-1 α-ethenyl-α-phe... CAS#:119-61-9 Benzophenone
CAS#:63645-18-1 4-hydroxy-4,4-d...
DownStream 0

HS Code	2933399090
Summary	2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Difenidol

1,1-diphenyl-4-piperidylbutanol

Vontrol

Nometic

1,1-diphenyl-4-piperidin-1-ylbutan-1-ol

DIPHENIDOL

defenidol

Difenidolo [DCIT]

Difenidolo

Cephadol

Difenidolum

Avomol

1,1-diphenyl-4-piperidin-1-yl-butan-1-ol

Difenidol

Use of Difenidol

Names

Difenidol Biological Activity

Chemical & Physical Properties

Toxicological Information

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

Safety Information

Synthetic Route

Precursor & DownStream

Customs

Synonyms