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On the Role of Ca++ Binding Proteins as Possible Targets for Ca++ Sensitizing Agents

On the Role of Ca++ Binding Proteins as Possible Targets for Ca++ Sensitizing Agents

J W Herzig, U Quast

Z Kardiol. 1992;81 Suppl 4:49-55.

PMID: 1290306

Abstract:

We describe the effects of various cardioactive compounds on the Ca++ activation of force production and ATPase activity in isolated contractile structures from mammalian heart and, in some cases, skeletal muscle. We show that: 1) the Ca++ sensitizing activity of APP 201-533 does not discriminate between cardiac and skeletal muscle and is, therefore, not based on interaction with cardiac troponin I phosphorylation at serine 20. 2) compounds like trifluoperazine or bepridil, both known to interact with calmodulin, increase the Ca++ sensitivity of the contractile structures of the heart, in high concentrations, as expected from the high natural abundance of troponin C. 3) DPI 201-106 interacts with calmodulin (and presumably with the structurally closely related troponin C) in the microM concentration range. Its high Ca(++)-sensitizing potency in skinned cardiac muscle and a certain sensitivity of this effect to the detergent Triton X-100 suggest accumulation of the hydrophobic compound in the myofibrillar protein lattice.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP62749262	Amrinone Related Compound C		62749-26-2	Price

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