Determinants of positive cooperativity between strychnine-like allosteric modulators and N-methylscopolamine at muscarinic receptors
Language English Country United States Media print
Document type Journal Article
PubMed
17192652
DOI
10.1385/jmn:30:1:111
PII: JMN:30:1:111
Knihovny.cz E-resources
- MeSH
- Allosteric Regulation MeSH
- Asparagine MeSH
- Protein Conformation MeSH
- Mutagenesis, Site-Directed MeSH
- N-Methylscopolamine pharmacology MeSH
- Proline MeSH
- Receptors, Muscarinic chemistry drug effects physiology MeSH
- Serine MeSH
- Strychnine pharmacology MeSH
- Amino Acid Substitution MeSH
- Threonine MeSH
- Valine MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Asparagine MeSH
- N-Methylscopolamine MeSH
- Proline MeSH
- Receptors, Muscarinic MeSH
- Serine MeSH
- Strychnine MeSH
- Threonine MeSH
- Valine MeSH
It has been shown previously that the third extracellular loop (o3) and its vicinity play a critical role in allosteric modulation at muscarinic acetylcholine receptors (mAChRs) (Ellis et al., 1993; Krejçí and Tuçek, 2001; Buller et al., 2002). In this study interaction of four chemically related substances (strychnine, its dimethoxy derivate brucine, precursor for synthesis of strychnine Wieland-Gumlich aldehyde (WGA), and precursor for synthesis of alcuronium propargyl-WGA) with orthosteric antagonist N-methylscopolamine (NMS) was investigated on the M3 subtype of mAChRs mutated at the o3 loop.
