Barnidipine hydrochloride

한글명:Barnidipine hydrochloride

카스 번호104757-53-1

상품명:Barnidipine hydrochloride

CBNumberCB1397277

분자식C27H30ClN3O6

포뮬러 무게528

MOL 파일104757-53-1.mol

화학적 성질

녹는점	223-226°C
알파	D20 +116.4° (c = 1 in methanol)
저장 조건	Sealed in dry,Room Temperature
용해도	insoluble in H2O; insoluble in EtOH; ≥16.3 mg/mL in DMSO with gentle warming
물리적 상태	결정성 고체
CAS 데이터베이스	104757-53-1(CAS DataBase Reference)

위험 및 안전 성명

독성

LD50 orally in male, female rats: 105, 113 mg/kg (Satoh)

NFPA 704:

	0
2		0

그림문자(GHS)

Barnidipine hydrochloride 화학적 특성, 용도, 생산

개요
Barnidipine hydrochloride, chemically known as (3S)-1-benzyl-3-pyrrolidinylmethyl-(4S)-2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate hydrochloride, is a new long-acting dihydropyridine calcium antagonist developed and marketed by Yamanouchi Pharmaceutical (now Astellas Pharma). This medication effectively lowers blood pressure without impacting heart rate by specifically targeting calcium channels responsible for transmembrane potential. By inhibiting calcium influx into cells, it selectively relaxes smooth muscle in peripheral and coronary blood vessels.
화학적 성질
Pale Yellow Solid. Melting point 226-228°C. [α]D20+116.4° (C=1, methanol). Insoluble in water. Acute toxicity LD50 male and female rats (mg/kg): 105, 113 Oral.
용도
Barnidipine hydrochloride is a vasodilating dihydropyridine calcium antagonist useful in the treatment of primary hypertension and renal hypertension. In experimental animals, its hypotensive effect was more potent and longer acting than nicardipine, nifedipine and nitrendipine.
정의
ChEBI: Barnidipine hydrochloride is a dihydropyridine. 1,4-Dihydropyridine calcium antagonist with antihypertensive and diuretic effects. It is a potential candidate in the treatment of patients with renal parenchymal hypertension.
생물학적 활성
Barnidipine is a dihydropyridine calcium channel blocker that has an IC50 value of 0.35 nM in potassium-induced tonic contraction of pig coronary artery. It demonstrates antihypertensive activity by reducing peripheral vascular resistance. It decreases blood pressure in spontaneously hypertensive rats when administered orally at 1 and 3 mg/kg per day. Formulations containing barnidipine have been used as a treatment for hypertension.
참고 문헌
[1] WEGENERJ W. Barnidipine block of L-type Ca(2+) channel currents in rat ventricular cardiomyocytes.[J]. British Journal of Pharmacology, 2000. DOI:10.1038/sj.bjp.0703514.
[2] ALP YILDIRIMF ILKAY. Barnidipine ameliorates the vascular and renal injury in L-NAME-induced hypertensive rats.[J]. European journal of pharmacology, 2015. DOI:10.1016/j.ejphar.2015.07.033.
[3] CHENGZHI-GANG. Synthesis and characterization of impurities of barnidipine hydrochloride, an antihypertensive drug substance.[J]. Molecules, 2014. DOI:10.3390/molecules19011344.

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