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Usage

Uses

Used in Pharmaceutical Industry:
Methoxyverapamil hydrochloride is used as a calcium channel antagonist for the treatment of various conditions, including cardiovascular diseases and certain parasitic infections. Its ability to block calcium entry in Schistosoma mansoni parasites makes it a potential candidate for combating parasitic infections.
Used in Cellular Research:
In cellular research, Methoxyverapamil hydrochloride is used as a calcium entry blocker in cultured macrophages. This application aids in studying the role of calcium signaling in immune cell function and the regulation of inflammatory responses.
Used in Neurological Research:
Methoxyverapamil hydrochloride is used in the inhibition of L-type voltage-gated Ca2+-channels, which are crucial for various neuronal functions. This application is valuable for investigating the role of calcium channels in neurological disorders and developing potential therapeutic agents.
Used in Reproductive Biology:
Methoxyverapamil hydrochloride impacts sperm capacitation function by affecting intracellular calcium levels. This makes it a useful tool in reproductive biology research, particularly in the study of sperm function and fertility treatments.

Biochem/physiol Actions

Blocks L-type Ca2+ channels

InChI:InChI=1/C28H40N2O5/c1-20(2)28(19-29,22-17-25(33-6)27(35-8)26(18-22)34-7)13-9-14-30(3)15-12-21-10-11-23(31-4)24(16-21)32-5/h10-11,16-18,20H,9,12-15H2,1-8H3

Upstream product

• 3490-06-0 N-methylhomoveratrylamine 
• 66332-86-3 α-(2-formylethyl)-α-isopropyl-3,4,5-trimethoxybenzeneacetonitrile 

Relevant academic research and scientific papers

THERAPY FOR COMPLICATIONS OF DIABETES

A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.

ANTIHYPERTENSIVE THERAPY

A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers.

Method for treating resistant hypertension

A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

Preparation of phenylacetonitriles carrying basic substituents

A process for the preparation of phenylacetonitriles, carrying basic substituents, of the formula I STR1 where R1, R2, R3, R4, R5, R6, R7 and R8 have the meanings given in the description, by reacting an aldehyde of the formula II STR2 with an amine of the formula III STR3