PMID

Data

Article Title

Organization

Challenges in the development of an M

Vanderbilt University Medical Center

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.

Vanderbilt University Medical Center

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

(S)-(-)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine maleate (SIB-1508Y): a novel anti-parkinsonian agent with selectivity for neuronal nicotinic acetylcholine receptors.

Sibia Neurosciences

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)

Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.

Novo Nordisk

 

Structure activity relationships of non-peptide bradykinin B2 receptor antagonists

TBA

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

 

Synthesis and binding affinity of new muscarinic ligands structurally related to oxotremorine

TBA

 

Identification of novel (isoxazole)methylene-1-azabicyclic compounds with high affinity for the central nicotinic cholinergic receptor

TBA

 

A rationale for the design and synthesis of m1 selective muscarinic agonists.

TBA

 

Synthesis and structure-activity relationships of heterocyclic analogues of the functional M₁ selective muscarinic agonist hexyloxy-TZTP

TBA

 

Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5

TBA

 

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

TBA

 

Cholinergic agents: 2-oxazolidinone analogues of the acetylcholine-receptor muscarinic agonist pilocarpine

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

Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.

Hoechst-Roussel Pharmaceuticals

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