Determinants of positive cooperativity between strychnine-like allosteric modulators and N-methylscopolamine at muscarinic receptors
Jazyk angličtina Země Spojené státy americké Médium print
Typ dokumentu časopisecké články
PubMed
17192652
DOI
10.1385/jmn:30:1:111
PII: JMN:30:1:111
Knihovny.cz E-zdroje
- MeSH
- alosterická regulace MeSH
- asparagin MeSH
- konformace proteinů MeSH
- mutageneze cílená MeSH
- N-methylskopolamin farmakologie MeSH
- prolin MeSH
- receptory muskarinové chemie účinky léků fyziologie MeSH
- serin MeSH
- strychnin farmakologie MeSH
- substituce aminokyselin MeSH
- threonin MeSH
- valin MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- asparagin MeSH
- N-methylskopolamin MeSH
- prolin MeSH
- receptory muskarinové MeSH
- serin MeSH
- strychnin MeSH
- threonin MeSH
- valin 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.
