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Pharmacological properties of oxotremorine and its analogs.
TLDR
A number of analogs of oxotremorine, including agonists, partial agonists and antagonists, are described, many of which are potent and highly specific in their central actions.
Structural requirements for muscarinic receptor occupation and receptor activation by oxotremorine analogs in the guinea-pig ileum.
  • B. Ringdahl
  • Chemistry, Medicine
    The Journal of pharmacology and experimental…
  • 1985
TLDR
There was no correlation between relative affinities and efficacies of the nine agonists studied, suggesting different structural requirements for occupation and activation of muscarinic receptors in the guinea-pig ileum, and some of the latter had substantially greater efficacy than oxotremorine.
Regional differences in receptor reserve for analogs of oxotremorine in vivo: implications for development of selective muscarinic agonists.
TLDR
Efficacious agonists appeared to have a large receptor reserve with respect to salivation, analgesia and hypothermia, whereas their receptor reserve for the tremor response was lower and the possibility is raised of achieving selective muscarinic actions by exploiting regional differences in receptor density, in the efficiency of receptor-effector coupling and in endogenous levels of acetylcholine.
Dissociation constants and relative efficacies of acetylcholine, (+)‐ and (‐)‐methacholine at muscarinic receptors in the guinea‐pig ileum
  • B. Ringdahl
  • Chemistry, Medicine
    British journal of pharmacology
  • 1 September 1986
TLDR
It is suggested that the methyl group at the chiral centre of (+)‐methacholine has no apparent effect on the binding to muscarinic receptors, whereas the corresponding methyl group of (‐)‐pig isolated ileum interferes with binding, presumably by stabilizing a conformation of the drug which does not fit the receptor very well.
The conversion of 2-chloroalkylamine analogues of oxotremorine to aziridinium ions and their interactions with muscarinic receptors in the guinea pig ileum.
TLDR
BM 123 and BM 130 are potent and specific muscarinic agonists that bind irreversibly to mus carinic receptors.
Muscarinic activity and receptor binding of the enantiomers of aceclidine and its methiodide.
TLDR
The enantiomeric potency ratios for the tremorogenic, analgesic, and sialogogic effects in mice agreed well with the ratio KH of (-)-ACEclidine/KH of (+)-aceclidine.
Muscarinic activity in the isolated guinea pig ileum of some carboxamides related to oxotremorine.
TLDR
The observation that the agonist N-(4-dimethylamino-2-butynyl)-N-methylpropionamide has a dissociation constant, estimated after elimination of spare receptors with dibenamine, suggests that the decrease in muscarinic agonist activity with increasing substitution is due mainly to a loss of efficacy.
5-Methyl-2-pyrrolidone analogues of oxotremorine as selective muscarinic agonists.
  • B. Ringdahl
  • Chemistry, Medicine
    Journal of medicinal chemistry
  • 1 March 1988
TLDR
A series of N-(4-amino-2-butynyl)-5-methyl- 2-pyrrolidones modified only in the amino group was synthesized, suggesting that the compounds had similar mode of binding to muscarinic receptors.
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