Efonidipine

Efonidipine (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].

111011-63-3

NZ-105; (±) -Efonidipine

12352005

H315, H317, H319, H335, H360

Calcium Channel

Reference compound

Membrane Transporter/Ion Channel; Neuronal Signaling

Neuroscience-Neuromodulation

Cardiovascular Disease

https://www.medchemexpress.com/Efonidipine.html

10mM

99.88

DMSO : 100 mg/mL (ultrasonic)

CC1=C(P2(OCC(C)(C)CO2)=O)C(C3=CC([N+]([O-])=O)=CC=C3)C(C(OCCN(C4=CC=CC=C4)CC5=CC=CC=C5)=O)=C(C)N1

C34H38N3O7P

631.66

H315, H317, H319, H335, H360

[1]Ikeda K, et al. Efonidipine, a Ca (2+) -channel blocker, enhances the production of dehydroepiandrosterone sulfate in NCI-H295R human adrenocortical carcinoma cells. Tohoku J Exp Med. 2011;224 (4) :263-71.|[2]Nakano N, et al. Effects of efonidipine, an L- and T-type calcium channel blocker, on the renin-angiotensin-aldosterone system in chronic hemodialysis patients. Int Heart J. 2010 May;51 (3) :188-92.|[3]Suzuki S, et al. Beneficial effects of the dual L- and T-type Ca2+ channel blocker efonidipine on cardiomyopathic hamsters. Circ J. 2007 Dec;71 (12) :1970-6.|[4]Lee TS, et al. Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78 (1) :11-20.

Room Temperature

-20°C, 3 years; 4°C, 2 years (Powder)

Reference compound1

Launched