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Efonidipine hydrochloride monoethanolate

CAS No. : 111011-76-8

Biological Activity：Efonidipine hydrochloride monoethanolate (NZ-105 hydrochloride monoethanolate) 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].

Research Area：Cardiovascular Disease

Targets：Calcium Channel

Related Screening Libraries:Drug Repurposing Compound Library Plus;FDA-Approved Drug Library Plus;FDA-Approved Drug Library Mini;Bioactive Compound Library Plus;Membrane Transporter/Ion Channel Compound Library;Neuronal Signaling Compound Library;FDA-Approved Drug Library;Drug Repurposing Compound Library;Anti-Cardiovascular Disease Compound Library;FDA Approved & Pharmacopeial Drug Library;Neuroprotective Compound Library;Calcium Channel Blocker Library;Human Metabolite Library;

Related Small Molecules:Benidipine hydrochloride;CaV1.3 antagonist-1;14-Deoxyandrographolide;(Rac)-MEM 1003;Glaucine;L-Ascorbic acid sodium salt;Brompheniramine-d6 maleate;MRS 1523;Nilvadipine;Lercanidipine;CP-060;Anipamil-d25 hydrochloride;ISX-9;ω-Conotoxin MVIIC;Catharanthine;Thapsigargin;Tetrandrine;Ginsenoside Rd;Manidipine dihydrochloride;ω-Agatoxin IVA;AE0047 Hydrochloride;PDE1-IN-4

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