Organic intermediate Methyldopa Powder

CAS:555-30-6

MF:C10H13NO4

MW:211.22

EINECS:209-089-2

Specification​: 99% min Methyldopa Powder

Sample:Methyldopa Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: white to off-white

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Methyldopa Usage and Synthesis.

Methyldopa, antihypertensive, alpha receptor agonist, commonly available in tablet form. It is an alpha-receptor that excites the vasomotor centre, thus inhibiting the external sympathetic nerves and producing a hypotensive effect, accompanied by slowing down of the heart rate, reduction of cardiac output, dilatation of small arteries, a significant reduction in peripheral vascular resistance, and an insignificant reduction in cardiac output when applied for a long period of time.

Clinical use for moderate, severe or malignant hypertension, especially for secondary hypertension, pregnancy hypertension, heart failure combined hypertension, coronary heart disease combined hypertension and elderly hypertensive patients.

Uses and functions of Methyldopa.

Methyldopa as an antihypertensive drug

Levomethodopa is a B-receptor blocking cardiovascular drug with good efficacy in moderate procedures of essential and renal hypertension.

It is used in moderate, severe or malignant hypertension, especially in renal hypertension or hypertension with renal dysfunction.

Pharmacological Effect of Methyldopa.

This product is an aromatic acid decarboxylase inhibitor. Only the levo-isomer of α-methyldopa has antihypertensive activity in humans, and the racemate (DL-α-methyldopa) requires twice the dose to achieve the same antihypertensive effect.

Its antihypertensive effect may be mediated by its active metabolite, β-methylnorepinephrine, which stimulates central inhibitory β-receptors and pseudo-neurotransmitters and reduces plasma renin activity, thereby lowering arterial blood pressure.

Methyldopa reduces tissue concentrations of 5-hydroxytryptamine, dopamine, norepinephrine, and metanephrines. It has no direct effect on cardiac function and usually does not reduce glomerular filtration rate, renal blood flow, or filtration fraction.

Cardiac output remained unchanged at normal heart rate, with some patients experiencing a slowing of the heart rate. Plasma renin activity is reduced during treatment.

Methyldopa reduces prone and standing blood pressure and rarely postural hypotension. Rarely hypotension during daytime exercise.

Production Method of  Bulk Methyldopa Powder.

Vanillin is methylated to veratraldehyde with dimethyl sulphate, then condensed with nitroethane to obtain 1-(2-nitropropenyl)-3',4'-dimethoxybenzene, which is reduced with iron powder and hydrolysed to produce 3',4'-dimethoxybenzopropiophenone (see 14945), and then by cyclization, ring-opening and hydrolysis to obtain DL-methyldopa, and the levulose is split to obtain methyldopa