105979-17-7 Usage
Description
Benidipine, with the CAS number 105979-17-7, is a 1,4-dihydropyridine calcium channel antagonist. It functions by blocking the movement of calcium ions into heart and blood vessel muscle cells, which results in the relaxation of blood vessels and a subsequent decrease in blood pressure.
Uses
Used in Pharmaceutical Industry:
Benidipine is used as an antihypertensive agent for the treatment of high blood pressure (hypertension). It helps to lower blood pressure by dilating blood vessels, which in turn reduces the resistance against the flow of blood, allowing the heart to pump more efficiently and with less strain.
Additionally, Benidipine may also be used in other cardiovascular applications due to its effects on calcium channels, which can have implications for conditions such as angina (chest pain) and certain types of arrhythmias (irregular heartbeats). However, the primary application of Benidipine remains its use as an antihypertensive medication.
Enzyme inhibitor
This oral, once-daily antihypertensive agent (FW = 505.57 g/mol; CAS 105979-17-7), also known by its code name KW-3049, trade name Coniel?, and systematic name O -methyl,O -[(3R)-1-(phenylmethyl)piperidin-3-yl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, is a dihydropyridine-class calcium ion blocker that is effective against L-, N-, and T-channels, with potent and selective inhibitory action on cardiac slow calcium channels. Benidipine bound stereospecifically to nitrendipine binding sites of rat myocardium with high affinity (Ki = 0.13 nM) and to the rat brain a1-adrenergic receptor (Ki = 1.2 μM). KW-3049 exhibited no remarkable binding affinity to a2 adrenergic, b-adrenergic, D2 dopamine, H1 histamine, S2 serotonin, A1 adenosine, A2 adenosine and muscarinic cholinergic receptors at 100 μM.
Check Digit Verification of cas no
The CAS Registry Mumber 105979-17-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,0,5,9,7 and 9 respectively; the second part has 2 digits, 1 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 105979-17:
(8*1)+(7*0)+(6*5)+(5*9)+(4*7)+(3*9)+(2*1)+(1*7)=147
147 % 10 = 7
So 105979-17-7 is a valid CAS Registry Number.
InChI:InChI=1/C28H31N3O6/c1-18-24(27(32)36-3)26(21-11-7-12-22(15-21)31(34)35)25(19(2)29-18)28(33)37-23-13-8-14-30(17-23)16-20-9-5-4-6-10-20/h4-7,9-12,15,23,26,29H,8,13-14,16-17H2,1-3H3/t23-,26-/m1/s1
105979-17-7Relevant articles and documents
THERAPY FOR COMPLICATIONS OF DIABETES
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, (2009/07/02)
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.
Synthesis and pharmacological activity of stereoisomers of 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl 1-(phenylmethyl)-3-piperidinyl ester
Muto,Kuroda,Kawato,Karasawa,Kubo,Nakamizo
, p. 1662 - 1665 (2007/10/02)
1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl 1-(phenylmethyl)-3-piperidinyl ester 1, a highly potent calcium antagonist, was separated into stereo- and optical isomers to investigate the differences of antihypertensive activities between them. Fractional crystallization of the hydrochlorides of 1 gave α- and β-diasterioisomers. The α-isomer (benidipine hydrochloride, KW-3049) showed very strong hypotensive effect, but little activity was observed in the β-isomer. From optically resolved 1,4-dihydro-5-methoxycarbonyl-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridi necarboxylic acids 2, and 1-benzyl-3-piperidinols 3, four optical isomers of 1 were synthesized, and their absolute configurations were deduced. The hypotensive activity of (+)-α, namely (S)-(S)-1, was 30 to 100 times stronger than that of (-)-α in intravenously administered spontaneously hypertensive rats.