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Molecular Pharmacology

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Abstract

N-methylanatoxinol isomers: derivatives of the agonist (+)-anatoxin-a block the nicotinic acetylcholine receptor ion channel.

K L Swanson, Y Aracava, F J Sardina, H Rapoport, R S Aronstam and E X Albuquerque
Molecular Pharmacology February 1989, 35 (2) 223-231;
K L Swanson
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Y Aracava
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F J Sardina
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H Rapoport
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R S Aronstam
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E X Albuquerque
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Abstract

Using biochemical and patch-clamp techniques, we investigated the pharmacology of S- and R-epimers of N-methylanatoxinol, which are analogs of the semi-rigid, stereoselective, nicotinic agonist (+)-anatoxin-a. In contrast to (+)-anatoxin-a, both isomers had poor ability to inhibit the binding of 125I-alpha-bungarotoxin or to open acetylcholine channels, and they were unable to elicit contracture of frog rectus abdominis muscles. However, both isomers were able to demonstrate significant concentration-dependent blockade of the nicotinic acetylcholine receptor ion channel. The R-isomer was approximately 4-fold more potent in causing inhibition of [3H]H12HTX binding than was the S-isomer, in the absence of carbamylcholine. In the presence of carbamylcholine, the affinity of the R-isomer of N-methylanatoxinol for the ion channel sites was further enhanced, so that its affinity became much greater than that of the S-isomer. Refinement of voltage- and concentration-dependent terms for the ion channel blocking and unblocking rates yielded functions that were able to predict the channel open times and short closed times well. The S-isomer bound and dissociated from the ion channel site of the nicotinic acetylcholine receptor more rapidly and with greater voltage sensitivity than the R-isomer. The present characterization of the antagonistic properties of these new analogs of (+)-anatoxin-a introduces a new aspect to the molecular pharmacology of (+)-anatoxin-a analogs; the semi-rigid compounds could be useful in describing the allosteric binding sites of the acetylcholine receptor, as well as in delimiting the agonist binding site.

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Molecular Pharmacology
Vol. 35, Issue 2
1 Feb 1989
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Abstract

N-methylanatoxinol isomers: derivatives of the agonist (+)-anatoxin-a block the nicotinic acetylcholine receptor ion channel.

K L Swanson, Y Aracava, F J Sardina, H Rapoport, R S Aronstam and E X Albuquerque
Molecular Pharmacology February 1, 1989, 35 (2) 223-231;

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Abstract

N-methylanatoxinol isomers: derivatives of the agonist (+)-anatoxin-a block the nicotinic acetylcholine receptor ion channel.

K L Swanson, Y Aracava, F J Sardina, H Rapoport, R S Aronstam and E X Albuquerque
Molecular Pharmacology February 1, 1989, 35 (2) 223-231;
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