化合物详情

CAS82586-55-8

分子式C25H30N2O5.HCl

分子量474.98 g/mol g/mol

危化品

Quinapril hydrochloride is a hydrochloride resulting from the reaction of equimolar amounts of quinapril and hydrogen chloride. A prodrug for quinaprilat hydrochloride (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) for the treatment of hypertension and congestive heart failure. It has a role as an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor and an antihypertensive agent. It contains a quinapril(1+).

科学粮草官-词典编辑部，修订于：2026-07-06

Toxicity

Symptoms

Overdose may lead to severe hypotension. The most common adverse effects observed in controlled clinical trials were dizziness, cough, chest pain, dyspnea, fatigue, and nausea/vomiting.

Interactions

Concurrent use /of other hypotension-producing medications/ with ACE inhibitors may produce additive hypotensive effects. /ACE inhibitors/ /Salt not specified/

Toxicity Data

LD<sub>50</sub>=1739mg/kg (orally in mice)

Exposure Routes

Peak plasma concentrations of quinapril occur within one hour following oral administration. The extent of absorption is at least 60%. The rate and extent of quinapril absorption are diminished moderately (approximately 25-30%) when ACCUPRIL tablets are administered during a high-fat meal.

Toxicity Summary

There are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a single polypeptide chain of 1277; and the testicular isoform, which has a lower molecular mass and is thought to play a role in sperm maturation and binding of sperm to the oviduct epithelium. Somatic ACE has two functionally active domains, N and C, which arise from tandem gene duplication. Although the two domains have high sequence similarity, they play distinct physiological roles. The C-domain is predominantly involved in blood pressure regulation while the N-domain plays a role in hematopoietic stem cell differentiation and proliferation. ACE inhibitors bind to and inhibit the activity of both domains, but have much greater affinity for and inhibitory activity against the C-domain. Qu...

Human Toxicity Excerpts

/SIGNS AND SYMPTOMS/ The principal adverse effect of ACE inhibitor overdose is hypotension, although hyperkalemia & renal failure may occur. ... /ACE inhibitors/ /Salt not specified/

Carcinogen Classification

No indication of carcinogenicity to humans (not listed by IARC).

Drug Induced Liver Injury

References: DOI:10.1016/j.drudis.2016.02.015

Non-Human Toxicity Values

LD50 in male, female mice, rats (mg/kg): 1739, 1840, 4280, 3541 orally; 504, 523, 158, 107 i.v. /Salt not specified/

Non-Human Toxicity Excerpts

/GENOTOXICITY/ Neither quinapril nor quinaprilat were mutagenic in the Ames bacterial assay with or without metabolic activation. Quinapril was also negative in the following genetic toxicology studies: in vitro mammalian cell point mutation, sister chromatid exchange in cultured cells, and in an in vivo cytogenetic study with rat bone marrow. /Salt not specified/

Antidote and Emergency Treatment

... Following gut decontamination, treatment is primarily supportive to maintain an adequate blood pressure. /ACE Inhibitors/ /Salt not specified/