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 |
27173801 |
29 |
Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration. |
Vanderbilt University Medical Center |
26191354 |
20 |
Pyrrolopyridine or Pyrazolopyridine Derivatives. |
Temple University |
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 |
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 |
| 7 |
6-Carboxymethyl-2-azabicyclo[2.2.1]heptane enantiomers: muscarinic activities of rigid analogues of arecoline |
TBA |
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 |
22546204 |
9 |
Recent developments and biological activities of thiazolidinone derivatives: a review. |
Dr. Hari Singh Gour University |
18178088 |
64 |
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. |
Vanderbilt Institute of Chemical Biology |
17034144 |
72 |
Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation. |
National Institute On Drug Abuse-Intramural Research Program |
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 |
15027858 |
35 |
Synthesis and monoamine transporter binding of 2-(diarylmethoxymethyl)-3 beta-aryltropane derivatives. |
University of New Orleans |
15189035 |
67 |
Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation. |
National Institute On Drug Abuse-Intramural Research Program |
12825932 |
61 |
Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter. |
National Institute On Drug Abuse |
11784139 |
82 |
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
Universit£ |
11170654 |
72 |
Structure-activity relationships at monoamine transporters and muscarinic receptors for N-substituted-3alpha-(3'-chloro-, 4'-chloro-, and 4',4''-dichloro-substituted-diphenyl)methoxytropanes. |
National Institute On Drug Abuse-Intramural Research Program |
11689080 |
43 |
Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues. |
National Institute of Diabetes and Digestive and Kidney Diseases |
10737741 |
50 |
Highly selective chiral N-substituted 3alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues for the dopamine transporter: synthesis and comparative molecular field analysis. |
National Institute On Drug Abuse-Intramural Research Program |
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 |
9083473 |
33 |
3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile. |
National Institutes of Health |
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 |
8765504 |
34 |
(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 |
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) |
7658434 |
52 |
Functionally selective M1 muscarinic agonists. 3. Side chains and azacycles contributing to functional muscarinic selectivity among pyrazinylazacycles. |
Eli Lilly |
8064804 |
3 |
Design, synthesis, and neurochemical evaluation of 2-amino-5-(alkoxycarbonyl)-3,4,5,6-tetrahydropyridines and 2-amino-5-(alkoxycarbonyl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists. |
University of Toledo |
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 |
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 |
15149693 |
56 |
The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor. |
National Institute On Drug Abuse-Intramural Research Program |
10450949 |
24 |
Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling. |
Wyeth-Ayerst Research |
| 28 |
Design of dual acting anticonvulsant-antimuscarinic succinimide and hydantoin derivatives |
TBA |
| 59 |
Muscarinic agonist SAR of azaspirodioxolanes |
TBA |
14695828 |
107 |
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
Universit£ |
22197142 |
42 |
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012. |
Vanderbilt University Medical Center |
21930376 |
92 |
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071. |
Vanderbilt University Medical Center |
21194936 |
39 |
Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe. |
Vanderbilt Institute of Chemical Biology/Chemical Synthesis Core |
19595599 |
14 |
Muscarinic receptor 1 agonist activity of novel N-aryl carboxamide substituted 3-morpholino arecoline derivatives in Alzheimer's presenile dementia models. |
University of Mysore |
20202841 |
47 |
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists. |
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 |
19717214 |
28 |
Synthesis and pharmacological evaluation of novel N-alkyl/aryl substituted thiazolidinone arecoline analogues as muscarinic receptor 1 agonist in Alzheimer's dementia models. |
University of Mysore |
| 20 |
Synthesis and binding affinity of new muscarinic ligands structurally related to oxotremorine |
TBA |
| 16 |
Identification of novel (isoxazole)methylene-1-azabicyclic compounds with high affinity for the central nicotinic cholinergic receptor |
TBA |
| 28 |
Acylhydrazones as M1/M3 selective muscarinic agonists |
TBA |
| 8 |
Synthesis and biological activity of enantiomers of a conformationally restricted muscarone analog |
TBA |
| 32 |
Synthesis and structure activity relationships of alkyl substituted analogues of the functional M1 selective muscarinic receptor agonist xanomeline |
TBA |
| 3 |
Muscarinic receptor probes based on amine congeners of pirenzepine and telenzepine |
TBA |
| 45 |
SR 46559 A and related aminopyridazines are potent muscarinic agonists with no cholinergic syndrome |
TBA |
| 21 |
Synthesis and structure-activity relationships of heterocyclic analogues of the functional M1 selective muscarinic agonist hexyloxy-TZTP |
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 |
18640043 |
20 |
Muscarinic receptor 1 agonist activity of novel N-arylthioureas substituted 3-morpholino arecoline derivatives in Alzheimer's presenile dementia models. |
University of Mysore |
18359231 |
18 |
Effect of novel N-aryl sulfonamide substituted 3-morpholino arecoline derivatives as muscarinic receptor 1 agonists in Alzheimer's dementia models. |
University of Mysore |
12729659 |
29 |
4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists. |
F. Hoffmann-La Roche |
11965364 |
36 |
Enantioselective synthesis of S-(+)-2beta-carboalkoxy-3alpha-[bis(4-fluorophenyl)methoxy]tropanes as novel probes for the dopamine transporter. |
National Institute On Drug Abuse-Intramural Research Program |
11934576 |
85 |
Synthesis and pharmacological evaluation of 6-piperidino- and 6-piperazinoalkyl-2(3H)-benzothiazolones as mixed sigma/5-HT(1A) ligands. |
Université |
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 |
9464368 |
78 |
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists. |
Eli Lilly |
9435902 |
60 |
Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter. |
National Institute On Drug Abuse |
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 |
8558530 |
4 |
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease. |
Hoechst-Roussel Pharmaceuticals |
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 |
7990109 |
62 |
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity. |
H. Lundbeck |
3373484 |
36 |
Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine. |
Dr. Karl Thomae |
2066986 |
137 |
Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine. |
Niddk |
1732522 |
42 |
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor. |
Sandoz Pharma |
1613751 |
68 |
Novel functional M1 selective muscarinic agonists. Synthesis and structure-activity relationships of 3-(1,2,5-thiadiazolyl)-1,2,5,6-tetrahydro-1-methylpyridines . |
Novo Nordisk Cns Division |
1613746 |
48 |
Synthesis and muscarinic receptor activity of ester derivatives of 2-substituted 2-azabicyclo[2.2.1]heptan-5-ol and -6-ol. |
Research Triangle Institute |
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 |
1548680 |
12 |
Synthesis and in vitro biological profile of all four isomers of the potent muscarinic agonist 3-(3-methyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane. |
Merck Sharp and Dohme Research Laboratories |
1433209 |
58 |
Novel functional M1 selective muscarinic agonists. 2. Synthesis and structure-activity relationships of 3-pyrazinyl-1,2,5,6-tetrahydro-1-methylpyridines. Construction of a molecular model for the M1 pharmacophore. |
Eli Lilly |
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 |