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Amlodipine Besylate

Amlodipine Besylate 구조식 이미지
카스 번호:
111470-99-6
상품명:
Amlodipine Besylate
동의어(영문):
Amlor;Vazkor;Amcard;Lowrac;Norvas;NORVASC;Amdepin;Amdipin;Amlodin;Amlopin
CBNumber:
CB4127875
분자식:
C26H31ClN2O8S
포뮬러 무게:
567.05094
MOL 파일:
111470-99-6.mol

Amlodipine Besylate 속성

녹는점
199-201°C
저장 조건
2-8°C
용해도
DMSO: 20 mg/mL
물리적 상태
solid
산도 계수 (pKa)
8.6
색상
white
수용성
Soluble in DMSO (20 mg/mL), water (10 mM), chloroform, ethanol (14 mg/mL), and methanol.
Merck
14,491
InChIKey
ZPBWCRDSRKPIDG-UHFFFAOYSA-N
CAS 데이터베이스
111470-99-6(CAS DataBase Reference)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 Xn
위험 카페고리 넘버 22-36/37/38-20/21/22
안전지침서 26-36
WGK 독일 3
RTECS 번호 US7967700
HS 번호 29333990
그림문자(GHS):
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H302 삼키면 유해함 급성 독성 물질 - 경구 구분 4 경고 P264, P270, P301+P312, P330, P501
H315 피부에 자극을 일으킴 피부부식성 또는 자극성물질 구분 2 경고 P264, P280, P302+P352, P321,P332+P313, P362
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 P264, P280, P305+P351+P338,P337+P313P
H335 호흡 자극성을 일으킬 수 있음 특정 표적장기 독성 - 1회 노출;호흡기계 자극 구분 3 경고
예방조치문구:
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P270 이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
P304+P340 흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
P405 밀봉하여 저장하시오.
P501 ...에 내용물 / 용기를 폐기 하시오.

Amlodipine Besylate C화학적 특성, 용도, 생산

개요

Anilodipine besylate is a new, once-daily, dihydropyridine calcium antagonist useful in the treatment of hypertension and angina.

화학적 성질

White Crystalline Solid

Originator

Pfizer (USA)

용도

A dihydropyridine calcium channel blocker. Used as an antianginal and antihypertensive

용도

Angiotensin II inhibitor prodrug, antihypertensive

용도

Amlodipine besylate is a L-type calcium channel blocker which may be used for the treatment of angina pectoris and hypertension. Amlodipine also inhibits growth of human epidermoid carcinoma A431 cells and has antireproductive effects in male rats.

정의

ChEBI: The benzenesulfonate salt of amlodipine.

Manufacturing Process

2-[(2-Aminoethoxy)methyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5- methoxycarbonyl-6-methyl-1,4-dihydropyridine (amlodipine) was prepared from 2-(phthalimidoaminoethoxy)acetoacetate, 2-chlorobenzaldehyde and methyl-3-aminocrotonate under refluxing in ethanol for 24 hours. The ketoester was prepared by the method of Troostwijk and Kellog (JCS Chem. Comm., 1977, p.932). Methyl-3-aminocrotonate can be prepared by known method. Phthalimido-amino-protecting group was removed using hydrazine hydrate in ethanol at the reflux temperature.
Although amlodipine is effective as the free base, in practice it is best administered form of a salt of a pharmaceutically acceptable acid.
Benzensulphonic salt of amlodipine was prepared as follows: Amlodipine base (65.6 g, 0.161 mols) was slurried in industrial methylated spirit (denatured alcohol, 326.4 ml) and cooled to 5°C. Benzensulphonic acid (26.2 g, 0.168 mols) was dissolved in industrial methylated spirit (65.6 ml) at 5°C and added to base. The resulting slurry was then granulated, filtered and washed with 2 volumes the same solvent (65.6 ml). The damp solid was slurred at 5°C for 1 hr in 327.6 ml industrial methylated spirit, filtered, washed with 2 volumes of the same solvent (65.6 ml) and dried under vacuum at 55°C for 24 hr. A yield of besylate salt of amlodipine 65 g.

상표명

Norvasc (Pfizer);Istin.

Therapeutic Function

Antianginal, Antihypertensive

생물학적 활성

L-type calcium channel blocker that displays antihypertensive properties. Inhibits Ca 2+ -induced contractions in depolarized rat aorta (IC 50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease. Inhibits proliferation of human vascular smooth muscle cells and epidermoid carcinoma A431 cells (IC 50 = 25 μ M).

Veterinary Drugs and Treatments

Oral amlodipine appears to be a useful agent in the treatment of hypertension in cats and many consider it the drug of choice for this indication. In pharmacokinetic studies, amlodipine has decreased blood pressure in dogs with chronic renal disease, but its efficacy in treating hypertensive dogs has been disappointing.
Hypertension in cats is usually secondary to other diseases (often renal failure or cardiac causes such as thyrotoxic cardiomyopathy or primary hypertrophic cardiomyopathy, etc.) and is most often seen in middle-aged or geriatric cats. These animals often present with acute clinical signs such as blindness, seizures, collapse or paresis. A cat is generally considered hypertensive if systolic blood pressure is >160 mmHg. Early reports indicate that if antihypertensive therapy is begun acutely, some vision may be restored in about 50% of cases of blindness secondary to hypertension.

Amlodipine Besylate 준비 용품 및 원자재

원자재

준비 용품


Amlodipine Besylate 공급 업체

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ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26725 60
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86-0551-65418684 18949823763
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18017610038
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