Diltiazem binding site

Schoemaker, H. and Langer, S.Z. (1985) [H-3] diltiazem binding to calcium-channel antagonists recognition sites in rat cerebral-cortex. European Journal of Pharmacology, 111, 273-277. 

Fig. 3 A model proposed by Corelli et al. for the binding of diltiazem-like CCBs with the receptor [38]. A hypothetical compound is shown to interact with a negative charge site, two hydrogen binding sites, and two hydrophobic sites of the receptor top view). Reprinted with permission from [38]. 1997 American Chemical Society... 

The specific Ca channel antagoni.sts verapamil, nifedipine, and diltiazem interact at specific sites on the calcium channel protein. These blockers do not occlude the channel physically but bind to sites in the channel, as they can promote both channel activation and antagonism. AITiniiy fix binding sites on the channel varies, depending un the status of the channel. The channel can exist in either an open (0. re.sting (R). or inactivated (I) state, and the equilibrium lx-, tween them is determined by stimulus frequency and mem-... 

Corelli F, Manetti F, Tafi A, Campiani G, Nacci V, Botta M. Diltiazem-like calcium entry blockers A hypothesis of the receptor-binding site based on a comparative molecular field analysis model. J Med Chem 1997 40 125-31. 

Bisbenzylisoquinoline alkaloids block Ca+2 uptake through L-type Ca+2 channel and modulate binding of ligands to four distinct sites (dihydropyridine, benzothiazepine, aralkylamine, and (diphenylbutyl)piperidine) in the Ca+2 entry blocker receptor complex of the channel. All bisbenzylisoquinoline analogs tested, including oxyacanthine, completely inhibit diltiazem binding,... 

Deng B, Lu H, Li L, Shi A, Kang Y, Xu Q (2010) Determination of the number of binding sites and binding constant between diltiazem hydrochloride and human serum albumin by ultrasonic microdialysis coupled with online capillary electrophoresis electrochemiluminescence. J Chromatogr A 1217(28) 4753-4756. doi 10.1016/j.chroma.2010.05.021... 

For example, in the case of compound XX, which among other activities has an IC50 of 60 nM on the calcium channel diltiazem site binding assay, a search for BioPrint compounds with an activity in the similar range yields a series of compounds nearly all of which are known calcium channel blockers (see Table 2.1). 

On searching the database among ADR associations we can retrieve a large number of associations for the calcium channel diltiazem site binding assay. Two ADR associations are shown in Figures 2.19 and 2.20. The ADR tinnitus has a... 

Table 2.1 BioPrint compounds with a similar strength hit on the calcium channel diltiazem site binding assay to compound XX.

Figure 7.12 Diagrammatic representation of cross section of calcium channel showing various sites that bind drugs and toxins. Bay K 8644, atrotoxin and maitotoxin are agonists (activators) of calcium channels. Nifedipine, verapamil, and diltiazem are antagonists (blockers) of calcium channels. (From Eldefrawi, M.E. and Eldefrawi, A.T., in Safe Insecticides Development and Use, Hodgson, E. and Kuhr, R.J., Eds., Marcel Dekker, New York, 1990, p. 155. With permission.)...

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