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. 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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 5 mg/mL|
Beneficial effects of the dual L- and T-type Ca2+ channel blocker efonidipine on cardiomyopathic hamsters.
Suzuki S,et.al. Circ J. 2007 Dec;1970-6. PMID: 18037756.
Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms.
Lee TS,et.al. Pharmacology. 2006;11-20. PMID: 16899990.
|Related Calcium Channel Products|
|Dantrolene sodium salt
Inhibitor of Ca2+ release from sarcoplasmic reticulum; muscle relaxant.
Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium-channel complexes in the CNS.
Ranolazine is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina.
L-Phenylalanine is an antagonist at α2δ calcium channels with a Ki of 980 nM.
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