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EFONIDIPINE HCL

EFONIDIPINE HCL structure

CAS No:
111011-53-1
Formula:
C34H38N3O7P.ClH
Chemical Name:
EFONIDIPINE HCL
Synonyms:
EFONIDIPINE HCL;Efonidipine hydrochloride;EFONIDIPINE HCL ETHANOL;3-Pyridinecarboxylicacid,5-(5,5-diMethyl-2-oxido-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-diMethyl-4-(3-nitrophenyl)-,2-[phenyl(phenylMethyl)aMino]ethyl ester, hydrochloride (1:1);2-(N-benzylanilino)ethyl5-(5,5-dimethyl-2-oxo-1,3,2λsup5sup-dioxaphosphinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylate,hydrochloride
Categories:
Chemical Reagents > Organic Reagents

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Description

EFONIDIPINE HCL Basic Attributes

Molecular Weight：

668.123

Exact Mass：

667.22100

Characteristics

PSA：

123

XLogP3：

8.95720

Melting Point：

169-170ºC

Boiling Point：

746.9ºC at 760 mmHg

Flash Point：

405.5ºC

Toxicity：

LD50 in mice (mg/kg): >600 orally (Seto)

Critical Temperature & Pressure：

Store at -20°C

Drug Information

MeSH：

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)|A class of drugs that act by selective inhibition of calcium influx through cellular membranes. (See all compounds classified as Calcium Channel Blockers.)|Agents that promote the excretion of urine through their effects on kidney function. (See all compounds classified as Diuretics.)

MeSH Entry Terms：

5-(5,5-dimethyl-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridinecarboxylic acid, 2-(phenyl(phenylmethyl)amino) ethyl ester, P-oxide, hydrochloride

EFONIDIPINE HCL Use and Manufacturing

Efonidipine Hcl (NZ-105) is a dual T-type and L-type calcium channel blocker (CCB). IC50 value: Target: calcium channel blocker in vitro: Efonidipine and nifedipine, but not other examined CCBs, also increased the N(6), 2'-O-dibutyryladenosine 3',5'-cyclic monophosphate (dbcAMP)-induced StAR mRNA, which reflects the action of adrenocorticotropic hormone, and efonidipine and R(-)-efonidipine enhanced the dbcAMP-induced DHEA-S production in NCI-H295R adrenocortical carcinoma cells [1]. I(Ca(T)) was blocked mainly by a tonic manner by nifedipine, by a use-dependent manner by mibefradil, and by a combination of both manners by efonidipine. IC50s of these Ca2+ channel antagonists to I(Ca(T)) and L-type Ca2+ channel current (I(Ca(L))) were 1.2 micromol/l and 0.14 nmol/l for nifedipine; 0.87 and 1.4 micromol/l for mibefradil, and 0.35 micromol/l and 1.8 nmol/l for efonidipine, respectively [4]. in vivo: Twenty hypertensive patients on chronic hemodialysis were given efonidipine 20-60 mg twice daily and amlodipine 2.5-7.5 mg once daily for 12 weeks each in a random crossover manner. The average blood pressure was comparable between the efonidipine and amlodipine periods (151 + or - 15/77 + or - 8 versus 153 + or - 15/76 + or - 8 mmHg). The pulse rate did not change significantly during the administration periods [2]. In the UM-X7.1 group, EFO treatment significantly attenuated the decrease of LVEF without affecting blood pressure compared with the vehicle group. EFO treatment decreased heart rate (by approximately 10%) in both groups [3].

Computed Properties

Molecular Weight:668.1
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:10
Exact Mass:667.2214153
Monoisotopic Mass:667.2214153
Topological Polar Surface Area:123
Heavy Atom Count:46
Complexity:1170
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes