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93 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Continued optimization of the MEBI
Vanderbilt University School Of Medicine
Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.EBI
Smithkline Beecham Pharmaceuticals
Phenyl-substituted analogues of oxotremorine as muscarinic antagonists.EBI
University Of Uppsala
Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands.EBI
Smithkline Beecham Pharmaceuticals
Comparison of azabicyclic esters and oxadiazoles as ligands for the muscarinic receptor.EBI
Smithkline Beecham Pharmaceuticals
Cholinergic activity of acetylenic imidazoles and related compounds.EBI
Upjohn
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.EBI
Ferrosan
Beta-lactam analogues of oxotremorine. 3- and 4-methyl-substituted 2-azetidinones.EBI
University Of Uppsala
Chemical and biochemical studies of 2-propynylpyrrolidine derivatives. Restricted-rotation analogues of N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide (BM-5).EBI
American Cyanamid
Synthesis of some 3-(1-azabicyclo[2.2.2]octyl) 3-amino-2-hydroxy-2-phenylpropionates: profile of antimuscarinic efficacy and selectivity.EBI
Nova Pharmaceutical
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.EBI
University Of Toledo
Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist.EBI
Johns Hopkins Medical Institutions
Conformationally restricted analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.EBI
University Of Uppsala
Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines.EBI
Kyowa Hakko Kogyo
Dimethylsulfonium and thiolanium analogues of the muscarinic agent oxotremorine.EBI
University Of California
Tricyclic compounds as selective antimuscarinics. 1. Structural requirements for selectivity toward the muscarinic acetylcholine receptor in a series of pirenzepine and imipramine analogues.EBI
TBA
Molecular modification of anticholinergics as probes for muscarinic receptors. 3. Conformationally restricted analogues of benactyzine.EBI
TBA
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.EBI
TBA
Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain.EBI
TBA
Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.EBI
TBA
Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain.EBI
TBA
Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogues.EBI
TBA
Challenges in the development of an MEBI
Vanderbilt University Medical Center
Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.EBI
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).EBI
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).EBI
Vanderbilt University
Discovery of ML326: The first sub-micromolar, selective M5 PAM.EBI
Vanderbilt University Medical Center
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.EBI
University Of Arkansas For Medical Sciences
Further exploration of M1 allosteric agonists: subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism.EBI
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.EBI
Vanderbilt University Medical Center
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.EBI
Vanderbilt Institute Of Chemical Biology
(S)-(-)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine maleate (SIB-1508Y): a novel anti-parkinsonian agent with selectivity for neuronal nicotinic acetylcholine receptors.EBI
Sibia Neurosciences
Design of potent non-peptide competitive antagonists of the human bradykinin B2 receptor.EBI
Sterling Winthrop Pharmaceutical Research Division
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.EBI
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues.EBI
Research Triangle Institute
Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics.EBI
Eli Lilly
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.EBI
Eli Lilly
Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.EBI
Royal Danish School Of Pharmacy
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.EBI
TBA
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.EBI
TBA
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.EBI
TBA
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.EBI
Novo Nordisk
 
Structure activity relationships of non-peptide bradykinin B2 receptor antagonistsEBI
TBA
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.EBI
Vanderbilt University Medical Center
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.EBI
Dvanderbilt Program In Drug Discovery
 
Synthesis and binding affinity of new muscarinic ligands structurally related to oxotremorineEBI
TBA
 
Identification of novel (isoxazole)methylene-1-azabicyclic compounds with high affinity for the central nicotinic cholinergic receptorEBI
TBA
 
A rationale for the design and synthesis of m1 selective muscarinic agonists.EBI
TBA
 
Synthesis and structure-activity relationships of heterocyclic analogues of the functional M1 selective muscarinic agonist hexyloxy-TZTPEBI
TBA
 
Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5EBI
TBA
 
Cholinergic agents: 2-oxazolidinone analogues of the acetylcholine-receptor muscarinic agonist pilocarpineEBI
TBA
Discovery of novel steroidal histamine HEBI
Chemical Works Of Gedeon Richter
Fluorination of Photoswitchable Muscarinic Agonists Tunes Receptor Pharmacology and Photochromic Properties.EBI
Julius Maximilian University Of W£Rzburg
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.EBI
Hoechst-Roussel Pharmaceuticals
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.EBI
Eli Lilly
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.EBI
National Institute Of Diabetes And Digestive And Kidney Diseases
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.EBI
University Of LièGe
Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.EBI
Universidade Federal Do Rio De Janeiro
cis-1,3,4,6,7,11b-Hexahydro-2-methyl-7-phenyl-2H-pyrazino[2,1-a] isoquinoline: a new atypical antidepressant.EBI
TBA
Synthesis, (18)F-labeling, and biological evaluation of piperidyl and pyrrolidyl benzilates as in vivo ligands for muscarinic acetylcholine receptors.EBI
University Of Michigan Medical School
Improving the nicotinic pharmacophore with a series of (Isoxazole)methylene-1-azacyclic compounds: synthesis, structure-activity relationship, and molecular modeling.EBI
Novo Nordisk
Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone.EBI
Astra Arcus Usa
Muscarinic analgesics with potent and selective effects on the gastrointestinal tract: potential application for the treatment of irritable bowel syndrome.EBI
Lilly Research Laboratories
In vitro muscarinic activity of spiromuscarones and related analogs.EBI
Fisons Pharmaceuticals
Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 2. 2-Phenoxy-, 2-(phenylthio)-, and 2-(phenylamino)alkanoic acid esters.EBI
Universit£
Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 1. Tropic and 2-phenylpropionic acid esters.EBI
Universit£
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.EBI
University Of Toledo
In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.EBI
TBA
A novel class of conformationally restricted heterocyclic muscarinic agonists.EBI
TBA
Ligand-Phospholipid Conjugation: A Versatile Strategy for Developing Long-Acting Ligands That Bind to Membrane Proteins by Restricting the Subcellular Localization of the Ligand.EBI
University Of Shizuoka
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.EBI
Warner-Lambert
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.EBI
TBA
Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.EBI
Vanderbilt University
Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists.EBI
Vanderbilt University School Of Medicine
Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.EBI
Vanderbilt University
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.EBI
Sandoz Pharma
Synthesis and muscarinic receptor activity of ester derivatives of 2-substituted 2-azabicyclo[2.2.1]heptan-5-ol and -6-ol.EBI
Research Triangle Institute
Optimization of MEBI
Vanderbilt University Medical Center
Urea and 2-imidazolidone derivatives of the muscarinic agents oxotremorine and N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.EBI
University Of Uppsala