The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27939174 |
84 |
Challenges in the development of an M |
Vanderbilt University Medical Center |
27185330 |
60 |
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 |
25147929 |
105 |
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 |
24164599 |
9 |
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 |
23562060 |
9 |
Discovery of ML326: The first sub-micromolar, selective M5 PAM. |
Vanderbilt University Medical Center |
23200253 |
67 |
Further exploration of M1 allosteric agonists: subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism. |
Vanderbilt University Medical Center |
23177787 |
59 |
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 |
9767650 |
48 |
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists. |
University of Bologna |
18178088 |
64 |
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. |
Vanderbilt Institute of Chemical Biology |
16250647 |
71 |
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. |
Universit£ |
9622546 |
109 |
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors. |
National Institute of Diabetes and Digestive and Kidney Diseases |
7562924 |
10 |
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) |
21930376 |
92 |
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071. |
Vanderbilt University Medical Center |
18059262 |
9 |
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. |
Dvanderbilt Program In Drug Discovery |
20004578 |
28 |
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 |
| 8 |
Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine. |
TBA |
19438238 |
45 |
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 |
31787491 |
54 |
Discovery of structurally distinct tricyclic M |
Vanderbilt University |
31784320 |
31 |
Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M |
Vanderbilt University |
27476142 |
104 |
Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition. |
Vanderbilt University School of Medicine |
31248774 |
45 |
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M |
Vanderbilt University |
30106578 |
10 |
Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts. |
TBA |
29652494 |
18 |
Ligand-Phospholipid Conjugation: A Versatile Strategy for Developing Long-Acting Ligands That Bind to Membrane Proteins by Restricting the Subcellular Localization of the Ligand. |
University of Shizuoka |
29037946 |
50 |
Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M |
Vanderbilt University |
2066986 |
137 |
Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine. |
Niddk |
28633897 |
73 |
Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists. |
Vanderbilt University School of Medicine |
28866269 |
61 |
Discovery of a novel, CNS penetrant M |
Vanderbilt University |
28442253 |
68 |
Optimization of M |
Vanderbilt University Medical Center |
28427812 |
74 |
Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype. |
Vanderbilt University School of Medicine |
23548908 |
1 |
Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis. |
University of Washington |
26051755 |
2 |
New monomeric and dimeric uridinyl derivatives as inhibitors of chitin synthase. |
Silesian University of Technology |