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Amlodipine

Amlodipine structure

CAS No:
88150-42-9
Formula:
C20H25ClN2O5
Chemical Name:
Amlodipine
Synonyms:
3,5-pyridinedicarboxylicacid,1,4-dihydro-2-((2-aminoethoxy)methyl)-4-(2-chlor;Amlodipine base (crystalline);(R)-3-ethyl 5-methyl 2;3-ethyl5-methylester;methyl ethyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate;AMLODIPINE;AMLODIPINE MM(CRM STANDARD);Amlodipine∬
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Amlodipine is a dihydropyridine L-type calcium channel blocker that selectively inhibits calcium influx in cardiac and vascular smooth muscle. Acting as a vasodilator, amlodipine reduces blood pressure by relaxing the smooth muscle in the arterial wall, decreasing total peripheral resistance. It inhibits calcium-induced contractions in depolarized rat aorta with an IC50value of 1.9 nM, displaying a slow rate of association and dissociation in isolated vascular and cardiac tissues. Amlodipine also demonstrates actions independent of L-type calcium channel blockade by regulating membrane fluidity and cholesterol deposition, stimulating nitric oxide production, acting as an antioxidant, and regulating matrix depositionin vitroandin vivo. Formulations containing amlodipine have been used in the treatment of hypertension.

Yellow Solid

Amlodipine was first patented in 1982 but approved as a prescription drug in 1990. Amlodipine is in the form of salt, the available salt forms are besilat, mesilate, and maleate. Amlodipine is an approved drug used to treat high blood pressure and coronary artery disease. Amlodipine is also sold under the brand name Norvasc. It was evaluated against diuretics in the treatment of hypertension and was found to be useful in controlling arterial pressure. In 2023, it was the fifth most commonly prescribed medication in the United States, with more than 68 million prescriptions.

ChEBI: A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina.

Amlodipine, 2-[, for the treatment of hypertension. Amlodipineis also marketed as a combination therapy with atorvastatinunder the tradename Norvasc for the management of highcholesterol and high blood pressure.

Amlodipine Basic Attributes

Molecular Weight：

408.88

EC Number：

1308068-626-2

Color/Form：

White

Characteristics

Density：

1.227±0.06 g/cm3(Predicted)

Melting Point：

178-179°C

Boiling Point：

527.2±50.0 °C(Predicted)

Water Solubility：

75.3 mg/L

Toxicity：

TDLo orl-chd: 400 mg/kg:BPR AJEMEN 18,581,2000

PKA：

pKa 8.6 (Uncertain)

Critical Temperature & Pressure：

Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

Safety Information

Hazard category：

IRRITANT

RTECS Number：

US7968329

Hazard Statements：

Human systemic effects.

RIDADR：

UN2811

Amlodipine Use and Manufacturing

A dihydropyridine calcium channel blocker; activity resides mainly in the (-)-isomer.

anti-hypertensive;calcium channel blocker

A deuterated dihydropyridine calcium channel blocker.;Application of Labeled APIs: Labeled Amlodipine, intended for use as an internal standard for the quantification of Amlodipine by GC- or LC-mass spectrometry.

Material

Ethanolamine

2-Chlorobenzaldehyde

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