Identification of binding sites for calcium channel antagonists. 1996

H Nakayama, and A Kuniyasu
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.

The binding sites of three typical calcium channel antagonists, 1, 4-dihydropyridines, benzothiazepines and phenylalkylamines, were successfully identified within the primary structures of calcium channels using a photoaffinity labeling technique. The results confirm pharmacological observations of the three antagonists that had been proposed to interact allosterically with each other. We briefly review the results and discuss the future prospects.

UI MeSH Term Description Entries
D002121 Calcium Channel Blockers A class of drugs that act by selective inhibition of calcium influx through cellular membranes. Calcium Antagonists, Exogenous,Calcium Blockaders, Exogenous,Calcium Channel Antagonist,Calcium Channel Blocker,Calcium Channel Blocking Drug,Calcium Inhibitors, Exogenous,Channel Blockers, Calcium,Exogenous Calcium Blockader,Exogenous Calcium Inhibitor,Calcium Channel Antagonists,Calcium Channel Blocking Drugs,Exogenous Calcium Antagonists,Exogenous Calcium Blockaders,Exogenous Calcium Inhibitors,Antagonist, Calcium Channel,Antagonists, Calcium Channel,Antagonists, Exogenous Calcium,Blockader, Exogenous Calcium,Blocker, Calcium Channel,Blockers, Calcium Channel,Calcium Blockader, Exogenous,Calcium Inhibitor, Exogenous,Channel Antagonist, Calcium,Channel Blocker, Calcium,Inhibitor, Exogenous Calcium
D004095 Dihydropyridines Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position.
D004110 Diltiazem A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions. Aldizem,CRD-401,Cardil,Cardizem,Dilacor,Dilacor XR,Dilren,Diltiazem Hydrochloride,Diltiazem Malate,Dilzem,Tiazac,CRD 401,CRD401
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000345 Affinity Labels Analogs of those substrates or compounds which bind naturally at the active sites of proteins, enzymes, antibodies, steroids, or physiological receptors. These analogs form a stable covalent bond at the binding site, thereby acting as inhibitors of the proteins or steroids. Affinity Labeling Reagents,Labeling Reagents, Affinity,Labels, Affinity,Reagents, Affinity Labeling
D001552 Benzazepines Compounds with BENZENE fused to AZEPINES.
D001665 Binding Sites The parts of a macromolecule that directly participate in its specific combination with another molecule. Combining Site,Binding Site,Combining Sites,Site, Binding,Site, Combining,Sites, Binding,Sites, Combining
D013841 Thiazepines Compounds that are derivatives of THIEPINS, with a nitrogen replacing a carbon in the seven-membered heterocyclic compound. Thiazepine
D014700 Verapamil A calcium channel blocker that is a class IV anti-arrhythmia agent. Iproveratril,Calan,Cordilox,Dexverapamil,Falicard,Finoptin,Isoptin,Isoptine,Izoptin,Lekoptin,Verapamil Hydrochloride,Hydrochloride, Verapamil

Related Publications

H Nakayama, and A Kuniyasu
October 1985, European journal of pharmacology,
H Nakayama, and A Kuniyasu
April 1991, European journal of pharmacology,
H Nakayama, and A Kuniyasu
May 1985, European journal of pharmacology,
H Nakayama, and A Kuniyasu
July 1991, American journal of hypertension,
H Nakayama, and A Kuniyasu
June 1992, Trends in pharmacological sciences,
H Nakayama, and A Kuniyasu
January 1994, Postgraduate medicine,
H Nakayama, and A Kuniyasu
August 1993, The Practitioner,
H Nakayama, and A Kuniyasu
September 1992, The Journal of pharmacology and experimental therapeutics,
Copied contents to your clipboard!