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 |
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 |
24837158 |
60 |
Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists. |
Astellas Pharma |
23375092 |
16 |
The effect of absolute configuration on activity, subtype selectivity (M3/M2) of 3a-acyloxy-6ß-acetoxyltropane derivatives as muscarinic M3 receptor antagonists. |
Shanghai Jiao Tong University |
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 |
12392730 |
10 |
Synthesis and muscarinic M(2) subtype antagonistic activity of enantiomeric pairs of 3-demethylhimbacine (3-norhimbacine) and its C(4)-epimer. |
Kyorin Pharmaceutical |
12270166 |
8 |
Synthesis and muscarinic M2 subtype antagonistic activity of unnatural ent-himbacine and an enantiomeric pair of (2'S,6'R)-diepihimbacine. |
Kyorin Pharmaceutical |
| 20 |
Design, synthesis and biological activity of some 4-DAMP- related compounds |
TBA |
18178088 |
64 |
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. |
Vanderbilt Institute of Chemical Biology |
17629699 |
42 |
Synthesis and optimization of novel and selective muscarinic M(3) receptor antagonists. |
Ranbaxy Research Laboratories |
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£ |
16220976 |
66 |
Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists. |
Astellas Pharma |
10354408 |
58 |
1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives. |
Novo Nordisk |
9464362 |
19 |
5-HT3 antagonists derived from aminopyridazine-type muscarinic M1 agonists. |
Universit£ |
9622546 |
109 |
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors. |
National Institute of Diabetes and Digestive and Kidney Diseases |
9572883 |
32 |
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties. |
University of Catania |
9016336 |
15 |
Stereoselective synthesis and biodistribution of potent [11C]-labeled antagonists for positron emission tomography imaging of muscarinic receptors in the airways. |
Groningen University Hospital |
7562926 |
81 |
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors. |
National Institutes of Health |
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) |
8027978 |
50 |
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds. |
Albany Molecular Research |
8464039 |
12 |
Synthesis and biodistribution of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate. A new ligand for the potential imaging of muscarinic receptors by single photon emission computed tomography. |
Oak Ridge National Laboratory |
8246221 |
90 |
The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives. |
Medical Research Division of American Cyanamid |
8360873 |
25 |
Synthesis and structure-activity studies of a series of spirooxazolidine-2,4-diones: 4-oxa analogues of the muscarinic agonist 2-ethyl-8-methyl-2,8-diazaspiro[4.5]decane-1,3-dione. |
Institute For Drug Discovery Research |
1956033 |
121 |
Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues. |
Research Triangle Institute |
1920350 |
22 |
Muscarinic receptor binding profile of para-substituted caramiphen analogues. |
Virginia Commonwealth University |
2374141 |
33 |
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads. |
Istituto De Angeli |
2738887 |
22 |
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates. |
Institute of Research |
3385735 |
32 |
Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists. |
Nova Pharmaceutical |
3385727 |
48 |
Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres. |
Royal Danish School of Pharmacy |
| 28 |
Design of dual acting anticonvulsant-antimuscarinic succinimide and hydantoin derivatives |
TBA |
21930376 |
92 |
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071. |
Vanderbilt University Medical Center |
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 |
| 20 |
Synthesis and binding affinity of new muscarinic ligands structurally related to oxotremorine |
TBA |
| 8 |
Synthesis and biological activity of enantiomers of a conformationally restricted muscarone analog |
TBA |
| 14 |
Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivity |
TBA |
| 24 |
Simplified analogs of himbacine displaying potent binding affinity for muscarinic receptors |
TBA |
| 3 |
Muscarinic receptor probes based on amine congeners of pirenzepine and telenzepine |
TBA |
| 40 |
Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5 |
TBA |
| 8 |
Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine. |
TBA |
| 14 |
Cholinergic agents: 2-oxazolidinone analogues of the acetylcholine-receptor muscarinic agonist pilocarpine |
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 |
15808475 |
40 |
Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine. |
Ranbaxy Research Laboratories |
12419388 |
25 |
Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification. |
Schering-Plough Research Institute |
32202101 |
120 |
Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists. |
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg |
10636243 |
6 |
Synthesis and binding studies of some epibatidine analogues. |
Institute of Pharmacy and Biochemistry |
10571170 |
27 |
Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors. |
Dipartimento Di Scienze Farmaceutiche - Università |
31074983 |
202 |
Conjugation of Short Peptides to Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Determines M |
University of Regensburg |
9572880 |
44 |
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand. |
University of Camerino |
8709107 |
99 |
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
Yamanouchi Pharmaceutical |
8558529 |
195 |
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 |
8246239 |
84 |
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives. |
Solvay Duphar |
7966137 |
52 |
Construction of a molecular shape analysis-three-dimensional quantitative structure-analysis relationship for an analog series of pyridobenzodiazepinone inhibitors of muscarinic 2 and 3 receptors. |
College of Pharmacy |
7837240 |
19 |
Preparation of 18F-labeled muscarinic agonist with M2 selectivity. |
National Institutes of Health |
23352509 |
27 |
Pharmacological properties and predicted binding mode of arylmethylene quinuclidine-like derivatives at the ?3?4 nicotinic acetylcholine receptor (nAChR). |
Targacept |
7752195 |
30 |
Syntheses and biological properties of chiral fluoroalkyl quinuclidinyl benzilates. |
National Institutes of Health |
9703467 |
84 |
Synthesis and pharmacological characterization of O-alkynyloximes of tropinone and N-methylpiperidinone as muscarinic agonists. |
National University of Singapore |
3373484 |
36 |
Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine. |
Dr. Karl Thomae |
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 |
2754696 |
56 |
Tricyclic compounds as selective muscarinic receptor antagonists. 3. Structure-selectivity relationships in a series of cardioselective (M2) antimuscarinics. |
Dr. Karl Thomae |
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 |
1588567 |
18 |
Synthesis and pharmacological investigation of the enantiomers of muscarone and allomuscarone. |
Istituto Chimico-Farmaceutico Dell'Università |
1578480 |
26 |
Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors. |
Abbott Laboratories |
28442253 |
68 |
Optimization of M |
Vanderbilt University Medical Center |
1507203 |
96 |
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
University of South Carolina |
23548908 |
1 |
Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis. |
University of Washington |
26390252 |
12 |
Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer. |
Dana-Farber Cancer Institute |
26218629 |
26 |
Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1). |
Oregon Health & Science University |
26214585 |
23 |
Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents. |
University of Wisconsin-Madison |
26364932 |
22 |
Structure and Inhibition of Microbiome ß-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity. |
University of North Carolina At Chapel Hill |
25590533 |
245 |
Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1. |
University of North Carolina At Chapel Hill |
26051755 |
2 |
New monomeric and dimeric uridinyl derivatives as inhibitors of chitin synthase. |
Silesian University of Technology |