| pubmed-article:2465486 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:2465486 | lifeskim:mentions | umls-concept:C0028778 | lld:lifeskim |
| pubmed-article:2465486 | lifeskim:mentions | umls-concept:C0243192 | lld:lifeskim |
| pubmed-article:2465486 | lifeskim:mentions | umls-concept:C0022009 | lld:lifeskim |
| pubmed-article:2465486 | lifeskim:mentions | umls-concept:C0034830 | lld:lifeskim |
| pubmed-article:2465486 | lifeskim:mentions | umls-concept:C0022203 | lld:lifeskim |
| pubmed-article:2465486 | lifeskim:mentions | umls-concept:C0283130 | lld:lifeskim |
| pubmed-article:2465486 | lifeskim:mentions | umls-concept:C0243072 | lld:lifeskim |
| pubmed-article:2465486 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:2465486 | pubmed:dateCreated | 1989-3-28 | lld:pubmed |
| pubmed-article:2465486 | pubmed:abstractText | 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. | lld:pubmed |
| pubmed-article:2465486 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:language | eng | lld:pubmed |
| pubmed-article:2465486 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:2465486 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2465486 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:2465486 | pubmed:month | Feb | lld:pubmed |
| pubmed-article:2465486 | pubmed:issn | 0026-895X | lld:pubmed |
| pubmed-article:2465486 | pubmed:author | pubmed-author:AronstamR SRS | lld:pubmed |
| pubmed-article:2465486 | pubmed:author | pubmed-author:AlbuquerqueE... | lld:pubmed |
| pubmed-article:2465486 | pubmed:author | pubmed-author:RapoportHH | lld:pubmed |
| pubmed-article:2465486 | pubmed:author | pubmed-author:SwansonK LKL | lld:pubmed |
| pubmed-article:2465486 | pubmed:author | pubmed-author:AracavaYY | lld:pubmed |
| pubmed-article:2465486 | pubmed:author | pubmed-author:SardinaF JFJ | lld:pubmed |
| pubmed-article:2465486 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:2465486 | pubmed:volume | 35 | lld:pubmed |
| pubmed-article:2465486 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:2465486 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:2465486 | pubmed:pagination | 223-31 | lld:pubmed |
| pubmed-article:2465486 | pubmed:dateRevised | 2007-11-15 | lld:pubmed |
| pubmed-article:2465486 | pubmed:meshHeading | pubmed-meshheading:2465486-... | lld:pubmed |
| pubmed-article:2465486 | pubmed:meshHeading | pubmed-meshheading:2465486-... | lld:pubmed |
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| pubmed-article:2465486 | pubmed:meshHeading | pubmed-meshheading:2465486-... | lld:pubmed |
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| pubmed-article:2465486 | pubmed:meshHeading | pubmed-meshheading:2465486-... | lld:pubmed |
| pubmed-article:2465486 | pubmed:meshHeading | pubmed-meshheading:2465486-... | lld:pubmed |
| pubmed-article:2465486 | pubmed:meshHeading | pubmed-meshheading:2465486-... | lld:pubmed |
| pubmed-article:2465486 | pubmed:meshHeading | pubmed-meshheading:2465486-... | lld:pubmed |
| pubmed-article:2465486 | pubmed:meshHeading | pubmed-meshheading:2465486-... | lld:pubmed |
| pubmed-article:2465486 | pubmed:year | 1989 | lld:pubmed |
| pubmed-article:2465486 | pubmed:articleTitle | N-methylanatoxinol isomers: derivatives of the agonist (+)-anatoxin-a block the nicotinic acetylcholine receptor ion channel. | lld:pubmed |
| pubmed-article:2465486 | pubmed:affiliation | Department of Pharmacology and Experimental Therapeutics, University of Maryland School of Medicine, Baltimore 21201. | lld:pubmed |
| pubmed-article:2465486 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:2465486 | pubmed:publicationType | In Vitro | lld:pubmed |
| pubmed-article:2465486 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| pubmed-article:2465486 | pubmed:publicationType | Research Support, U.S. Gov't, Non-P.H.S. | lld:pubmed |
| pubmed-article:2465486 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
