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Article Title

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Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.

Smithkline Beecham Pharmaceuticals

Phenyl-substituted analogues of oxotremorine as muscarinic antagonists.

University Of Uppsala

Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands.

Smithkline Beecham Pharmaceuticals

Comparison of azabicyclic esters and oxadiazoles as ligands for the muscarinic receptor.

Smithkline Beecham Pharmaceuticals

Cholinergic activity of acetylenic imidazoles and related compounds.

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.

Ferrosan

Beta-lactam analogues of oxotremorine. 3- and 4-methyl-substituted 2-azetidinones.

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).

American Cyanamid

Synthesis of some 3-(1-azabicyclo[2.2.2]octyl) 3-amino-2-hydroxy-2-phenylpropionates: profile of antimuscarinic efficacy and selectivity.

Nova Pharmaceutical

Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.

University Of Toledo

Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist.

Johns Hopkins Medical Institutions

Conformationally restricted analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.

University Of Uppsala

Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines.

Kyowa Hakko Kogyo

Dimethylsulfonium and thiolanium analogues of the muscarinic agent oxotremorine.

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.

TBA

Molecular modification of anticholinergics as probes for muscarinic receptors. 3. Conformationally restricted analogues of benactyzine.

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.

TBA

Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain.

TBA

Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.

TBA

Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain.

TBA

Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogues.

TBA

Challenges in the development of an M

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).

Vanderbilt University Medical Center

Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists.

Astellas Pharma

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

Further exploration of M1 allosteric agonists: subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism.

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.

Vanderbilt University Medical Center

Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.

University Of Bologna

 

Design, synthesis and biological activity of some 4-DAMP- related compounds

TBA

Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.

Vanderbilt Institute Of Chemical Biology

Synthesis and optimization of novel and selective muscarinic M(3) receptor antagonists.

Ranbaxy Research Laboratories

Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists.

Astellas Pharma

6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.

National Institute Of Diabetes And Digestive And Kidney Diseases

(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist.

Astra Arcus

(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

3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).

Hoechst-Roussel Pharmaceuticals

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

Design of potent non-peptide competitive antagonists of the human bradykinin B2 receptor.

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.

National Institute Of Diabetes And Digestive And Kidney Diseases

Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues.

Research Triangle Institute

Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.

Istituto De Angeli

Functionalized congener approach for the design of novel muscarinic agents. Synthesis and pharmacological evaluation of N-methyl-N-[4-(1-pyrrolidinyl)-2-butynyl] amides.

Niddk

Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.

Pfizer

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

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

Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.

Royal Danish School Of Pharmacy

Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.

TBA

Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.

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.

TBA

Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.

Novo Nordisk

 

Structure activity relationships of non-peptide bradykinin B2 receptor antagonists

TBA

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

Vanderbilt University Medical Center

 

Synthesis and binding affinity of new muscarinic ligands structurally related to oxotremorine

TBA

 

Serotonin 5-HT₄ agonist activity of a series of meso-azanoradamantane benzamides

TBA

 

Identification of novel (isoxazole)methylene-1-azabicyclic compounds with high affinity for the central nicotinic cholinergic receptor

TBA

 

A rationale for the design and synthesis of m1 selective muscarinic agonists.

TBA

 

Synthesis and structure-activity relationships of heterocyclic analogues of the functional M₁ selective muscarinic agonist hexyloxy-TZTP

TBA

 

Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5

TBA

 

Cholinergic agents: 2-oxazolidinone analogues of the acetylcholine-receptor muscarinic agonist pilocarpine

TBA

Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine.

Ranbaxy Research Laboratories

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

1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.

University Of Camerino

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

3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.

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.

National Institute Of Diabetes And Digestive And Kidney Diseases

Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.

Solvay Duphar

New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.

University Of LièGe

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

Neurochemistry of aging. 1. Toxins for an animal model of Alzheimer's disease.

TBA

In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.

TBA

A novel class of conformationally restricted heterocyclic muscarinic agonists.

TBA

Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.

Warner-Lambert

(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.

TBA

Tricyclic compounds as selective muscarinic receptor antagonists. 3. Structure-selectivity relationships in a series of cardioselective (M2) antimuscarinics.

Dr. Karl Thomae

Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.

Vanderbilt University

Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine.

Niddk

Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.

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.

Sandoz Pharma

Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.

Pfizer

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

Synthesis and pharmacological investigation of the enantiomers of muscarone and allomuscarone.

Istituto Chimico-Farmaceutico Dell'Università

Urea and 2-imidazolidone derivatives of the muscarinic agents oxotremorine and N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.

University Of Uppsala

Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis.

University Of Washington

New monomeric and dimeric uridinyl derivatives as inhibitors of chitin synthase.

Silesian University Of Technology