CAS 74764-40-2|Bepridil hydrochloride
| Common Name | Bepridil hydrochloride | ||
|---|---|---|---|
| CAS Number | 74764-40-2 | Molecular Weight | 421.01600 |
| Density | / | Boiling Point | / |
| Molecular Formula | C24H37ClN2O2 | Melting Point | 91 ±2° |
| MSDS | USA | Flash Point | / |
Names
| Name | bepridil hydrochloride monohydrate |
|---|---|
| Synonym | More Synonyms |
Bepridil hydrochloride BiologicalActivity
| 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 ChannelResearch 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 |
| InChIKey | UEECHQPWQHYEDE-UHFFFAOYSA-N |
| SMILES | CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1.Cl.O |
| Storage condition | Desiccate at RT |
Toxicological Information
CHEMICAL IDENTIFICATION |
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 |
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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 |
