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82857-38-3

82857-38-3 structure
82857-38-3 structure
  • Name: Bopindolol Malonate
  • Chemical Name: 1-[(2-Methyl-1H-indol-4-yl)oxy]-3-[(2-methyl-2-propanyl)amino]-2- propanyl benzoate
  • CAS Number: 82857-38-3
  • Molecular Formula: C23H28N2O3
  • Molecular Weight: 380.48000
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2017-03-11 10:22:37
  • Modify Date: 2023-02-01 11:10:10
  • Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol malonate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol malonate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol malonate is a prodrug of Pindolol (HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research[1][2][3][4].
Name 1-[(2-Methyl-1H-indol-4-yl)oxy]-3-[(2-methyl-2-propanyl)amino]-2- propanyl benzoate
Description Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol malonate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol malonate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol malonate is a prodrug of Pindolol (HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research[1][2][3][4].
Related Catalog
Target

Adrenergic receptor, Renin, 5-HT receptors[1][4]
In Vivo Bopindolol (intravenous injection; 8, 16 and 32 μg/kg) causes a dose-dependent inhibition of isoprenaline-induced tachycardia, and this agent is 4 times more potent than propranolol in anaesthetised dogs[1]. Bopindolol (0.3, 1 and 3 mg/kg; IP; single dosage) produces dose dependent decreases in diastolic blood pressure and in heart rate[2]. Animal Model: Male Wistar rats (260-300 g)[2] Dosage: 0.3, 1 and 3 mg/kg Administration: IP; single dosage Result: Produced dose dependent decreases in diastolic blood pressure, and the decrease of about 8 mmHg at 3 mg/kg. Decreased the heart rate in a dose-dependent manner.
References

[1]. Harron DW, et al. Bopindolol. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy. Drugs. 1991 Jan;41(1):130-49.

[2]. H Tanaka, et al. Hypotensive effect of bopindolol in pithed rats. Gen Pharmacol. 1993 Mar;24(2):373-5.

[3]. Y Hosohata, et al. Bopindolol is a slowly dissociating beta 1-adrenoceptor antagonist when compared to other beta-blockers. Biol Pharm Bull. 1995 Aug;18(8):1066-71.

[4]. Nagatomo T, et al. Bopindolol: pharmacological basis and clinical implications. Cardiovasc Drug Rev. 2001 Spring;19(1):9-24.
Molecular Formula C23H28N2O3
Molecular Weight 380.48000
Exact Mass 380.21000
PSA 63.35000
LogP 4.85970

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TY1844000
CAS REGISTRY NUMBER :
82857-38-3
LAST UPDATED :
199109
DATA ITEMS CITED :
3
MOLECULAR FORMULA :
C23-H28-N2-O3.C3-H4-O4
MOLECULAR WEIGHT :
484.60

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 :
824 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - convulsions or effect on seizure threshold Gastrointestinal - ulceration or bleeding from stomach
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,4369,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
481 mg/kg
TOXIC EFFECTS :
Behavioral - ataxia Lungs, Thorax, or Respiration - cyanosis Skin and Appendages - hair
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,4369,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9200 ug/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,4369,1989

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title: CAS No. 82857-38-3 | Chemsrc address: https://www.chemsrc.com/en/baike/181785.html

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