EurekaMag
+ Translate
+ Most Popular
The pigeon tick (Argas reflexus): its biology, ecology, and epidemiological aspects
Prevalence of hemoglobin abnormalities in Kebili (Tunisian South)
Lipogranuloma: a preventable complication of dacryocystorhinostomy
Value of basal plasma cortisol assays in the assessment of pituitary-adrenal insufficiency
Bees from the Belgian Congo. The acraensis group of Anthophora
Placing gingival retraction cord
Total serum IgE, allergy skin testing, and the radioallergosorbent test for the diagnosis of allergy in asthmatic children
Acariens plumicoles Analgesoidea parasites des oiseaux du Maroc
Injuries of terminal phalanges of the fingers in children
Biology of flowering and nectar production in pear (Pyrus communis)
Das Reliktvorkommen der Aspisviper (Vipera aspis L.) im Schwarzwald
Hydrological modelling of drained blanket peatland
Pathologic morphology and clinical significance of the anomalous origin of the left circumflex coronary artery from the right coronary artery. General review and autopsy analysis of 30 cases
Cyto genetic analyses of lymphocyte cultures after exposure to calcium cyclamate
Axelrodia riesei, a new characoid fish from Upper Rio Meta in Colombia With remarks concerning the genus Axelrodia and description of a similar, sympatric, Hyphessobrycon-species
Favorable evolution of a case of tuberculosis of pancreas under antibiotic action
RIFM fragrance ingredient safety assessment, Valencene, CAS Registry Number 4630-07-3
Parenteral microemulsions: an overview
Temperate pasture: management for grazing and conservation
Evaluation of a new coprocessed compound based on lactose and maize starch for tablet formulation
Thermal expansion and cracking of three confined water-saturated igneous rocks to 800C
Revision of the genera of the tribe Stigmoderini (Coleoptera: Buprestidae) a discussion of phylogenetic relationships
Anal tuberculosis. Report of a case
Gastric tuberculosis in the past and present
Adaptive responses of the cardiovascular system to prolonged spaceflight conditions: assessment with Holter monitoring

Allosteric interactions required for high-affinity binding of dihydropyridine antagonists to Ca(V)1.1 Channels are modulated by calcium in the pore


Allosteric interactions required for high-affinity binding of dihydropyridine antagonists to Ca(V)1.1 Channels are modulated by calcium in the pore



Molecular Pharmacology 70(2): 667-675



ISSN/ISBN: 0026-895X

PMID: 16675661

DOI: 10.1124/mol.105.020644

Dihydropyridines (DHPs) are an important class of drugs, used extensively in the treatment of angina pectoris, hypertension, and arrhythmia. The molecular mechanism by which DHPs modulate Ca2+ channel function is not known in detail. We have found that DHP binding is allosterically coupled to Ca2+ binding to the selectivity filter of the skeletal muscle Ca2+ channel Ca(V)1.1, which initiates excitation-contraction coupling and conducts L-type Ca2+ currents.

Please choose payment method:






(PDF emailed within 0-6 h: $19.90)

Accession: 011741015

Download citation: RISBibTeXText

Related references

Calcium binding in the pore of L-type calcium channels modulates high affinity dihydropyridine binding. Journal of Biological Chemistry 270(31): 18201-18204, 1995

Molecular determinants critical for the high affinity and allosteric modulation of dihydropyridine binding to L-type calcium channels. Biophysical Journal 70(2 Part 2): A185, 1996

Molecular determinants of high affinity dihydropyridine binding in L-type calcium channels. Journal of Biological Chemistry 271(10): 5293-5296, 1996

High affinity specific [3H](+)PN 200-110 binding to dihydropyridine receptors associated with calcium channels in rat cerebral cortex and heart. Life Sciences 35(7): 721-732, 1984

Allosteric interactions at L-type calcium channels between FPL 64176 and the enantiomers of the dihydropyridine Bay K 8644. Journal of Pharmacology and Experimental Therapeutics 275(2): 638-645, 1995

High affinity potassium binding in voltage-gated calcium-modulated channels. Biophysical Journal 76(1 Part 2): A188, 1999

Competitive binding experiments reveal differential interactions for dihydropyridine calcium channel activators and antagonists at dihydropyridine receptors on mouse brain membranes. Canadian Journal of Physiology and Pharmacology 72(7): 738-745, 1994

Calcicludine binding to the outer pore of L-type calcium channels is allosterically coupled to dihydropyridine binding. Biochemistry 46(25): 7590-7598, 2007

Labeling by [3H]1,3-di(2-tolyl)guanidine of two high affinity binding sites in guinea pig brain: evidence for allosteric regulation by calcium channel antagonists and pseudoallosteric modulation by sigma ligands. Molecular Pharmacology 39(2): 222-232, 1991

(-)-3H-desmethoxyverapamil labelling of putative calcium channels in brain: autoradiographic distribution and allosteric coupling to 1,4-dihydropyridine and diltiazem binding sites. Naunyn-Schmiedeberg's Archives of Pharmacology 327(2): 183-187, 1984

Correlation of binding affinity and pharmacologic potency for the dihydropyridine calcium antagonists in vascular smooth muscle. Clinical Research 34(2): 399A, 1986

Molecular determinants of cardiac Ca2+ channel pharmacology. Subunit requirement for the high affinity and allosteric regulation of dihydropyridine binding. Journal of Biological Chemistry 270(45): 27106-27111, 1995

Interactions of organic calcium channel antagonists with calcium channels in isolated frog atrial cells test of a modulated receptor hypothesis. Biophysical Journal 45(2 Part 2): 50A, 1984

Coordination of Ca2+ by the pore region glutamates is essential for high-affinity dihydropyridine binding to the cardiac Ca2+ channel a1 subunit. Biochemistry (American Chemical Society) 34: 50-5, 1995

Chemical and immunological characterization of binding sites for tetrodotoxin and dihydropyridine that are in close proximity to the external mouth of ion pore in the sodium and calcium channels. Protein Journal 11(4): 395-396, 1992