The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 1560440 |
42 |
Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives. |
Smithkline Beecham Pharmaceuticals |
| 1732545 |
27 |
Phenyl-substituted analogues of oxotremorine as muscarinic antagonists. |
University of Uppsala |
| 1619616 |
94 |
Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands. |
Smithkline Beecham Pharmaceuticals |
| 1895293 |
44 |
Comparison of azabicyclic esters and oxadiazoles as ligands for the muscarinic receptor. |
Smithkline Beecham Pharmaceuticals |
| 1875333 |
132 |
Cholinergic activity of acetylenic imidazoles and related compounds. |
Upjohn |
| 1995893 |
81 |
Muscarinic cholinergic agonists and antagonists of the 3-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,2,5,6-tetrahydropyridine type. Synthesis and structure-activity relationships. |
Ferrosan |
| 2299626 |
18 |
Beta-lactam analogues of oxotremorine. 3- and 4-methyl-substituted 2-azetidinones. |
University of Uppsala |
| 2258905 |
135 |
Chemical and biochemical studies of 2-propynylpyrrolidine derivatives. Restricted-rotation analogues of N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide (BM-5). |
American Cyanamid |
| 2296026 |
12 |
Synthesis of some 3-(1-azabicyclo[2.2.2]octyl) 3-amino-2-hydroxy-2-phenylpropionates: profile of antimuscarinic efficacy and selectivity. |
Nova Pharmaceutical |
| 2724292 |
120 |
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations. |
University of Toledo |
| 2785211 |
18 |
Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist. |
Johns Hopkins Medical Institutions |
| 2704032 |
10 |
Conformationally restricted analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide. |
University of Uppsala |
| 3351856 |
3 |
Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines. |
Kyowa Hakko Kogyo |
| 3336015 |
8 |
Dimethylsulfonium and thiolanium analogues of the muscarinic agent oxotremorine. |
University of California |
| 3039133 |
9 |
Tricyclic compounds as selective antimuscarinics. 1. Structural requirements for selectivity toward the muscarinic acetylcholine receptor in a series of pirenzepine and imipramine analogues. |
TBA |
| 3806613 |
2 |
Molecular modification of anticholinergics as probes for muscarinic receptors. 3. Conformationally restricted analogues of benactyzine. |
TBA |
| 2866248 |
8 |
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
TBA |
| 7108902 |
18 |
Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain. |
TBA |
| 6128416 |
29 |
Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems. |
TBA |
| 7288815 |
18 |
Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. |
TBA |
| 6249933 |
12 |
Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogues. |
TBA |
| 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 |
| 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 |
| 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) |
| 8394936 |
11 |
Design of potent non-peptide competitive antagonists of the human bradykinin B2 receptor. |
Sterling Winthrop Pharmaceutical Research Division |
| 1319493 |
31 |
Synthesis and receptor binding properties of fluoro- and iodo-substituted high affinity sigma receptor ligands: identification of potential PET and SPECT sigma receptor imaging agents. |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 1956033 |
121 |
Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues. |
Research Triangle Institute |
| 2573732 |
84 |
Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. |
Eli Lilly |
| 2571731 |
33 |
Synthesis and pharmacological evaluation of CNS activities of [1,2,3]triazolo[4,5-b][1,5]-, imidazolo[4,5-b][1,5]-, and pyrido[2,3-b][1,5]benzodiazepines. 10-Piperazinyl-4H-1,2,3-triazolo[4,5-b][1,5]benzodiazepines with neuroleptic activity. |
Eli Lilly |
| 3385727 |
48 |
Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres. |
Royal Danish School of Pharmacy |
| 3039136 |
328 |
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships. |
TBA |
| 2869146 |
72 |
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
TBA |
| 6134835 |
76 |
Synthesis and receptor binding studies relevant to the neuroleptic activities of some 1-methyl-4-piperidylidene-9-substituted-pyrrolo[2,1-b][3]benzazepine derivatives. |
TBA |
| 9873644 |
74 |
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation. |
Novo Nordisk |
| | 40 |
Structure activity relationships of non-peptide bradykinin B2 receptor antagonists |
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 |
| 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 |
| | 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 |
| | 88 |
A rationale for the design and synthesis of m1 selective muscarinic agonists. |
TBA |
| | 21 |
Synthesis and structure-activity relationships of heterocyclic analogues of the functional M1 selective muscarinic agonist hexyloxy-TZTP |
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 |
| 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 |
| 31492518 |
40 |
Discovery of novel steroidal histamine H |
Chemical Works of Gedeon Richter |
| 31248774 |
45 |
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M |
Vanderbilt University |
| 30827105 |
23 |
Fluorination of Photoswitchable Muscarinic Agonists Tunes Receptor Pharmacology and Photochromic Properties. |
Julius Maximilian University of W£Rzburg |
| 30106578 |
10 |
Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts. |
TBA |
| 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 |
| 8410999 |
81 |
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
Eli Lilly |
| 8355251 |
8 |
Synthesis and binding properties of MK-801 isothiocyanates; (+)-3-isothiocyanato-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten- 5,10-imine hydrochloride: a new, potent and selective electrophilic affinity ligand for the NMDA receptor-coupled phencyclidine binding site. |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 8101877 |
80 |
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
University of LièGe |
| 23792350 |
53 |
Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
Universidade Federal Do Rio De Janeiro |
| 11087580 |
31 |
Synthesis, (18)F-labeling, and biological evaluation of piperidyl and pyrrolidyl benzilates as in vivo ligands for muscarinic acetylcholine receptors. |
University of Michigan Medical School |
| 10585207 |
31 |
Improving the nicotinic pharmacophore with a series of (Isoxazole)methylene-1-azacyclic compounds: synthesis, structure-activity relationship, and molecular modeling. |
Novo Nordisk |
| 9784090 |
11 |
Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone. |
Astra Arcus Usa |
| 9046345 |
20 |
Muscarinic analgesics with potent and selective effects on the gastrointestinal tract: potential application for the treatment of irritable bowel syndrome. |
Lilly Research Laboratories |
| 7739014 |
23 |
In vitro muscarinic activity of spiromuscarones and related analogs. |
Fisons Pharmaceuticals |
| 8201606 |
2 |
Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 2. 2-Phenoxy-, 2-(phenylthio)-, and 2-(phenylamino)alkanoic acid esters. |
Universit£ |
| 8201605 |
3 |
Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 1. Tropic and 2-phenylpropionic acid esters. |
Universit£ |
| 8464038 |
14 |
Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists. |
University of Toledo |
| 3746815 |
15 |
In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin. |
TBA |
| 3712371 |
49 |
A novel class of conformationally restricted heterocyclic muscarinic agonists. |
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 |
| 2892936 |
21 |
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines. |
Warner-Lambert |
| 2875184 |
57 |
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
TBA |
| 29037946 |
50 |
Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M |
Vanderbilt University |
| 2571728 |
21 |
Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. |
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 |
| 1967652 |
27 |
Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. |
Vanderbilt University |
| 28866269 |
61 |
Discovery of a novel, CNS penetrant M |
Vanderbilt University |
| 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 |
| 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 |
| 28442253 |
68 |
Optimization of M |
Vanderbilt University Medical Center |
| 1507212 |
42 |
Urea and 2-imidazolidone derivatives of the muscarinic agents oxotremorine and N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide. |
University of Uppsala |
| 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 |
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