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Muscarinic Interactions of Bisindolylmaleimide Analogues

Muscarinic Interactions of Bisindolylmaleimide Analogues

S Lazareno, A Popham, N J Birdsall

Eur J Pharmacol. 1998 Nov 6;360(2-3):281-4.

PMID: 9851596

Abstract:

We have used radioligand binding studies to determine the affinities of seven bisindolylmaleimide analogues, six of which are selective inhibitors of protein kinase C, at human muscarinic M1-M4 receptors. The compounds were most potent at M1 receptors, and Ro-31-8220 was the most potent analogue, with a Kd of 0.6 microM at M1 receptors. The weakest compounds, bisindolylmaleimide IV and bisindolylmaleimide V, had Kd values of 100 microM. If it is necessary to use protein kinase C inhibitors at concentrations of 10 microM or more in studies involving muscarinic receptors then bisindolylmaleimide IV may be the most appropriate inhibitor to use.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP119139230-A	Bisindolylmaleimide IV		119139-23-0	Price

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