| pubmed-article:8182702 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:8182702 | lifeskim:mentions | umls-concept:C0034826 | lld:lifeskim |
| pubmed-article:8182702 | lifeskim:mentions | umls-concept:C1709060 | lld:lifeskim |
| pubmed-article:8182702 | lifeskim:mentions | umls-concept:C1552603 | lld:lifeskim |
| pubmed-article:8182702 | lifeskim:mentions | umls-concept:C1706202 | lld:lifeskim |
| pubmed-article:8182702 | lifeskim:mentions | umls-concept:C0599740 | lld:lifeskim |
| pubmed-article:8182702 | pubmed:issue | 10 | lld:pubmed |
| pubmed-article:8182702 | pubmed:dateCreated | 1994-6-14 | lld:pubmed |
| pubmed-article:8182702 | pubmed:abstractText | The bis(dichlorobenzyl) ether of the bispyridinium oxime TMB 4 stabilizes antagonist binding to M2-cholinoceptors which is indicative of an allosteric action. More than 10 derivatives of the lead compound were synthesized to investigate structure-activity relationships. The allosteric potency of the compounds was indicated by the concentrations which retarded the rate of dissociation of [3H]N-methylscopolamine from porcine cardiac cholinoceptors by a factor of 2 (EC50). Compared with TMB 4, the bis(dichlorobenzyl) derivative 4a displayed a more than 200-fold higher potency (EC50 = 4.7 microM). One of the dichlorobenzyl groups could be replaced by a methyl group without loss of activity (EC50 = 4.5 microM). Further shortening of this end of the molecule was accompanied by a moderate decline in potency to a minimum of EC50 = 26 microM. The second quaternary nitrogen was not a prerequisite for an allosteric activity. It is concluded that one half of the lead compound is pivotal for an interaction with the allosteric site of the M2-cholinoceptor, whereas the opposite end of the molecule modulates the allosteric activity. | lld:pubmed |
| pubmed-article:8182702 | pubmed:language | eng | lld:pubmed |
| pubmed-article:8182702 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8182702 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:8182702 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8182702 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8182702 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8182702 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8182702 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:8182702 | pubmed:month | May | lld:pubmed |
| pubmed-article:8182702 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:8182702 | pubmed:author | pubmed-author:MohrKK | lld:pubmed |
| pubmed-article:8182702 | pubmed:author | pubmed-author:HolzgrabeUU | lld:pubmed |
| pubmed-article:8182702 | pubmed:author | pubmed-author:KostenisEE | lld:pubmed |
| pubmed-article:8182702 | pubmed:author | pubmed-author:TränkleCC | lld:pubmed |
| pubmed-article:8182702 | pubmed:author | pubmed-author:Botero CidM... | lld:pubmed |
| pubmed-article:8182702 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:8182702 | pubmed:day | 13 | lld:pubmed |
| pubmed-article:8182702 | pubmed:volume | 37 | lld:pubmed |
| pubmed-article:8182702 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:8182702 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:8182702 | pubmed:pagination | 1439-45 | lld:pubmed |
| pubmed-article:8182702 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
| pubmed-article:8182702 | pubmed:meshHeading | pubmed-meshheading:8182702-... | lld:pubmed |
| pubmed-article:8182702 | pubmed:meshHeading | pubmed-meshheading:8182702-... | lld:pubmed |
| pubmed-article:8182702 | pubmed:meshHeading | pubmed-meshheading:8182702-... | lld:pubmed |
| pubmed-article:8182702 | pubmed:meshHeading | pubmed-meshheading:8182702-... | lld:pubmed |
| pubmed-article:8182702 | pubmed:meshHeading | pubmed-meshheading:8182702-... | lld:pubmed |
| pubmed-article:8182702 | pubmed:meshHeading | pubmed-meshheading:8182702-... | lld:pubmed |
| pubmed-article:8182702 | pubmed:meshHeading | pubmed-meshheading:8182702-... | lld:pubmed |
| pubmed-article:8182702 | pubmed:meshHeading | pubmed-meshheading:8182702-... | lld:pubmed |
| pubmed-article:8182702 | pubmed:meshHeading | pubmed-meshheading:8182702-... | lld:pubmed |
| pubmed-article:8182702 | pubmed:meshHeading | pubmed-meshheading:8182702-... | lld:pubmed |
| pubmed-article:8182702 | pubmed:meshHeading | pubmed-meshheading:8182702-... | lld:pubmed |
| pubmed-article:8182702 | pubmed:year | 1994 | lld:pubmed |
| pubmed-article:8182702 | pubmed:articleTitle | Search for the pharmacophore of bispyridinium-type allosteric modulators of muscarinic receptors. | lld:pubmed |
| pubmed-article:8182702 | pubmed:affiliation | Institute of Pharmacy, University of Bonn, FRG. | lld:pubmed |
| pubmed-article:8182702 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:8182702 | pubmed:publicationType | In Vitro | lld:pubmed |
| pubmed-article:8182702 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:8182702 | lld:chembl |
