PMID

Data

Article Title

Organization

Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).

Vanderbilt University Medical Center

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375).

Vanderbilt University

Discovery of ML326: The first sub-micromolar, selective M5 PAM.

Vanderbilt University Medical Center

Further exploration of M1 allosteric agonists: subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism.

Vanderbilt University Medical Center

Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia.

Vanderbilt University Medical Center

Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.

University Of Bologna

Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.

Vanderbilt Institute Of Chemical Biology

6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.

National Institute Of Diabetes And Digestive And Kidney Diseases

Resolution and in vitro and initial in vivo evaluation of isomers of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate: a high-affinity ligand for the muscarinic receptor.

Oak Ridge National Laboratory (Ornl)

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

Vanderbilt University Medical Center

An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.

Dvanderbilt Program In Drug Discovery

Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.

Vanderbilt University Medical Center

 

Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine.

TBA

Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.

Vanderbilt University Medical Center

Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine.

Niddk

Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis.

University Of Washington

New monomeric and dimeric uridinyl derivatives as inhibitors of chitin synthase.

Silesian University Of Technology