Calcium channel agonists

O.V. Shishkin, Conformational flexibility of the 1, 4-dihydropyridine ring in calcium channel agonists and antagonists molecules. J. Mol. Stmct. 385, 209-214 (1996)... 

Among the former group, receptors that act as calcium ion or chloride ion channels play a crucial role in epidermal permeability barrier homeostasis. Topical application of calcium channel agonists delays the barrier recovery, while antagonists accelerate barrier repair.1,2,3 Topical application of chloride ion channel agonists accelerates the barrier recovery.2,4 The results of our studies are summarized in Table 15.1. 

QSAR studies of calcium channel agonists and antagonists can be viewed as useful tools for assessment of potential toxicity. Information on the primary structure of calcium channels has become increasingly accessible since their sequencing and 3D molecular models can be developed. Models based on the solved X-ray structure from the homologous voltage-gated potassium channel... 

Davis AM, Gensmantel NP, Johansson E, Marriott DP. The use of the GRID program in the 3-D QSAR analysis of a series of calcium-channel agonists. J Med Chem 1994 37 963-72. 

Ivanciuc, O., Ivanciuc, T. and Cabrol-Bass, D. (2000b) 3D quantitative structure-activity relationships with CoRSA. Comparative receptor surface analysis. Application to calcium channel agonists. Analusis, 28, 637—642. 

Such a compound can be viewed as calcium channel agonist. 

Yokoyama, A., et al., Some chemical properties of maitotoxin, a putative calcium channel agonist isolated from amarine dinoflageUate. J Bio chem (Tokyo), 1988 104(2) 184—187. 

Shan R, Velazquez C, Knaus EE (2004) Syntheses, calcium channel agonist-antagonist modulation activities, and nitric oxide release studies of nitrooxyalkyl l,4-dihydro-2,6-dimethyl-3-nitro-4-(2,l,3-benzoxadiazol-4-yl)pyridine-5-carboxylate racemates, enantiomers, and diastereomers. J Med Chem 47 254-261... 

Simons and Pocock (1987) obtained similar results in a study of lead uptake by adrenal medullary cells. They found that metal influx was stimulated by depolarizing the cells in high external K, but that the stimulated influx was blocked by methoxyverapamil (D600) with an affinity that was higher than that for blockade of Ca " influx (0.4 vs. 4.7//M). Lead uptake was stimulated by the calcium channel agonist BAY-K8644. As was seen with cadmium, these results are consistent with the notion that voltage-dependent calcium channels could be an important route for the entry of lead into cells. Pb permeation was not affected if Cl was replaced by NO, an observation consistent with the relatively low affinity of Pb " for... 

The Use of the GRID Program in the 3D-QSAR Analysis of a Series of Calcium-Channel Agonists. 

Mazzotta, J. B. Nguyen, D. Ebens, A. J. Winslow, J. Recombinant cell and method for identifying insect cyclic nucleotide-gated calcium channel agonists for use as insecti-cides. Ger. Offen. DE 102004062273, 2006 Chem. Abstr. 2006, 145, 120011. 

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