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972-02-1

972-02-1 structure
972-02-1 structure
  • Name: Difenidol
  • Chemical Name: diphenidol
  • CAS Number: 972-02-1
  • Molecular Formula: C21H27NO
  • Molecular Weight: 309.44500
  • Catalog: API Digestive system medication Antiemetic emetic
  • Create Date: 2018-08-31 17:26:30
  • Modify Date: 2024-01-08 14:27:36
  • 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
Synonyms 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
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
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
110-89-4 structure

110-89-4

201230-82-2 structure

201230-82-2

3923-51-1 structure

3923-51-1

~10%

972-02-1 structure

972-02-1

Literature: Schmidt, Andreas; Marchetti, Mauro; Eilbracht, Peter Tetrahedron, 2004 , vol. 60, # 50 p. 11487 - 11492
119-61-9 structure

119-61-9

~%

972-02-1 structure

972-02-1

Literature: Helvetica Chimica Acta, , vol. 24, p. 209 E, 220 E Journal of the American Chemical Society, , vol. 74, p. 4085
110-89-4 structure

110-89-4

63645-18-1 structure

63645-18-1

~%

972-02-1 structure

972-02-1

Literature: Journal of Organometallic Chemistry, , vol. 332, p. 9 - 18
110-89-4 structure

110-89-4

~%

972-02-1 structure

972-02-1

Literature: GB683950 , ;
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%

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