<Suppliers Price>

Bepridil hydrochloride

Names

[ CAS No. ]:
74764-40-2

[ Name ]:
Bepridil hydrochloride

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Melting Point ]:
91 ±2°

[ Molecular Formula ]:
C24H37ClN2O2

[ Molecular Weight ]:
421.01600

[ Exact Mass ]:
420.25400

[ PSA ]:
24.94000

[ LogP ]:
5.50580

[ Appearance of Characters ]:
powder | white

[ Storage condition ]:
Desiccate at RT

MSDS

Toxicological Information

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

Safety Information

[ 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

Articles

Pulsed infrared radiation excites cultured neonatal spiral and vestibular ganglion neurons by modulating mitochondrial calcium cycling.

J. Neurophysiol. 112(6) , 1246-55, (2014)

Cochlear implants are currently the most effective solution for profound sensorineural hearing loss, and vestibular prostheses are under development to treat bilateral vestibulopathies. Electrical cur...

A recoverable state of axon injury persists for hours after spinal cord contusion in vivo.

Nat. Commun. 5 , 5683, (2014)

Therapeutic strategies for spinal cord injury (SCI) commonly focus on regenerating disconnected axons. An alternative approach would be to maintain continuity of damaged axons, especially after contus...

Serum flecainide S/R ratio reflects the CYP2D6 genotype and changes in CYP2D6 activity.

Drug Metab. Pharmacokinet. 30 , 257-62, (2015)

The aims of this study were to clarify whether the ratio of S- to R-flecainide (S/R ratio) in the serum flecainide concentration was associated with the stereoselectivity of flecainide metabolism, and...


More Articles


Related Compounds