J-104129, a novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors.

@article{Mitsuya1999J104129AN,
  title={J-104129, a novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors.},
  author={Morihiro Mitsuya and Toshiaki Mase and Yoshimi Tsuchiya and Kumiko Kawakami and Hanae Hattori and K. Kobayashi and Yoshio Ogino and Toru Fujikawa and Atsushi Satoh and T. Kimura and Kazuhito Noguchi and Norikazu Ohtake and K Tomimoto},
  journal={Bioorganic \& medicinal chemistry},
  year={1999},
  volume={7 11},
  pages={
          2555-67
        }
}
Discovery of 2-aminothiazole-4-carboxamides, a novel class of muscarinic M(3) selective antagonists, through solution-phase parallel synthesis.
TLDR
In the course of searching for a muscarinic M(3) antagonist with a structure distinct from those of the 2-(4,4-difluorocyclopentyl)-2-phenylacetamide derivatives, a thiazole-4-carboxamide derivative was identified as a lead compound in the in-house chemical collection.
A new series of M3 muscarinic antagonists based on the 4-amino-piperidine scaffold.
Novel, highly selective, muscarinic M3 receptor antagonists
  • Biology, Chemistry
  • 2001
A series of muscarinic receptor antagonists based upon a polyamide backbone linking a trityl group and a N-alkylpiperidine, or N,N-dialkylpiperidinium group, are claimed. The linking group may be
1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.
Functional activation of G-proteins coupled with muscarinic acetylcholine receptors in rat brain membranes.
TLDR
All of the data suggest that functional activation of Gi/o proteins coupled to mAChRs, especially the M4 subtype, is detectable by means of CCh-stimulated [(35)S]GTPγS binding assay in rat discrete brain regions.
Medicinal chemistry and therapeutic potential of muscarinic M3 antagonists
TLDR
The introduction of selective M3 antagonists has not improved clinical efficacy compared with the old non‐selective antimuscarinics but has reduced the rate of adverse events mediated by the blockade of cardiac M2 receptors (tachycardia) and central M1 receptors (cognitive impairment).
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