74764-40-2

74764-40-2 structure

Name: Bepridil hydrochloride
Chemical Name: bepridil hydrochloride monohydrate
CAS Number: 74764-40-2
Molecular Formula: C₂₄H₃₇ClN₂O₂
Molecular Weight: 421.01600
Catalog: API Circulatory system medication Prevention and treatment of angina pectoris
Create Date: 2018-09-15 05:43:24
Modify Date: 2024-01-08 21:12:12
Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca+ channel antagonist and Na+, K+ channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na+/Ca2+ exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders[1][2][3][4][5].

Name	bepridil hydrochloride monohydrate
Synonyms	3-isobutoxy-2-pyrrolidino-n-phenyl-n-benzylpropylaminehydrochloridehydrate MFCD00065498 Unii-4W2p15D93m l)-,monohydrochloride,monohydrate angopril Bepridil hydrochloride,N-Benzyl-N-(3-isobutoxy-2-pyrrolidin-1-yl-propyl)anilinehydrochloride

Description	Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca+ channel antagonist and Na+, K+ channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na+/Ca2+ exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders[1][2][3][4][5].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Cardiovascular Disease
Target	Ca2+
In Vitro	Bepridil hydrochloride hydrate blockades of Ca2+-dependent action potentials in vascular smooth muscle of dog coronary artery[2]. Bepridil hydrochloride hydrate blocks Ca currents and Na currents with IC50s of 0.5 μM and 30 μM, respectively in cultured ventricular cells[4]. Bepridil hydrochloride hydrate decreases IKs under blockade of IKr with E4031 (5 μM), in a concentration-dependent manner[5].
In Vivo	Bepridil hydrochloride hydrate exhibits a half-life of averages 33±15 hours after single-dose administration[6].
References	[1]. A Gill, et al. Pharmacology of Bepridil. Am J Cardiol. 1992 Apr 9;69(11):11D-16D. [2]. D R Harder, et al. Bepridil Blockade of Ca2+-dependent Action Potentials in Vascular Smooth Muscle of Dog Coronary Artery. J Cardiovasc Pharmacol. Jul-Aug 1981;3(4):906-14. [3]. Yasuhide Watanabe. Cardiac Na +/Ca 2+ Exchange Stimulators Among Cardioprotective Drugs. J Physiol Sci. 2019 Nov;69(6):837-849. [4]. A Yatani, et al. Bepridil Block of Cardiac Calcium and Sodium Channels. J Pharmacol Exp Ther. 1986 Apr;237(1):9-17. [5]. J C Wang, et al. Bepridil Differentially Inhibits Two Delayed Rectifier K(+) Currents, I(Kr) and I(Ks), in Guinea-Pig Ventricular Myocytes. Br J Pharmacol. 1999 Dec;128(8):1733-8. [6]. L Z Benet, et al. Pharmacokinetics and Metabolism of Bepridil. Am J Cardiol. 1985 Mar 15;55(7):8C-13C.

Melting Point	91 ±2°
Molecular Formula	C₂₄H₃₇ClN₂O₂
Molecular Weight	421.01600
Exact Mass	420.25400
PSA	24.94000
LogP	5.50580
Appearance	powder \| white
Storage condition	Desiccate at RT

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UY1162000

CHEMICAL NAME :: 1-Pyrrolidineethanamine, beta-((2-methylpropoxy)methyl)-N-phenyl-N-(phenylmeth yl)-, monohydrochloride, monohydrate

CAS REGISTRY NUMBER :: 74764-40-2

LAST UPDATED :: 199506

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C24-H34-N2-O.Cl-H.H2-O

MOLECULAR WEIGHT :: 421.08

WISWESSER LINE NOTATION :: T5NTJ AY1O1Y1&1&1NR&1R &GH &QH

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 :: 6850 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,682,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,682,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >21300 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,682,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1955 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: GWXXBX German Offenlegungsschrift Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2802864

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,682,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 23500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: GWXXBX German Offenlegungsschrift Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2802864

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes	Xi
RIDADR	NONH for all modes of transport
WGK Germany	2
RTECS	UY1162000

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