PMID

Data

Article Title

Organization

Phenyl-substituted analogues of oxotremorine as muscarinic antagonists.

University Of Uppsala

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

Resolved pyrrolidine, piperidine, and perhydroazepine analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.

Uppsala University

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

University Of Uppsala

Dimethylsulfonium and thiolanium analogues of the muscarinic agent oxotremorine.

University Of California

6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.

TBA

Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.

University Of Mainz

Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH

Jagiellonian University Medical College

Challenges in the development of an M

Vanderbilt University Medical Center

Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.

University Of Kansas

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

Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.

Jagiellonian University Medical College

Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.

University Of Illinois At Chicago

Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.

City University Of New York

Muscarinic acetylcholine receptor binding affinities of pethidine analogs.

University Of Kentucky

Molecular hybridization yields triazole bronchodilators for the treatment of COPD.

Pfizer

Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M1 agonists.

Eli Lilly

Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.

Universit£

Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.

Vanderbilt University Medical Center

Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).

Universit£

2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.

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 arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.

Adamed

Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide.

Universit£

Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.

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.

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

The discovery of new spirocyclic muscarinic M3 antagonists.

Astrazeneca

The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists.

Glaxosmithkline

2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR.

Glaxosmithkline

2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.

Glaxosmithkline

Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.

Universit£

Synthesis, affinity profile and functional activity of potent chiral muscarinic antagonists with a pyrrolidinylfuran structure.

Universita Di Firenze

Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.

Universit£

Muscarinic antagonists with multiple stereocenters: Synthesis, affinity profile and functional activity of isomeric 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine sulfoxide derivatives.

Universit£

As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).

The University Of Sydney

Synthesis and biological characterization of a series of novel diaryl amide M1 antagonists.

Vanderbilt University Medical Center

Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.

TBA

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.

Vanderbilt University Medical Center

Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.

H. Lundbeck

Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.

Vanderbilt University Medical Center

1,4-dioxane, a suitable scaffold for the development of novel M3 muscarinic receptor antagonists.

Universit£

7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands.

The University Of Sydney

Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.

National Institute Of Mental Health

Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.

Vanderbilt University Medical Center

Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.

National Institute Of Mental Health

Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.

H. Lundbeck

High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.

Purdue University

Design and synthesis of a fluorescent muscarinic antagonist.

Pfizer

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Abbott Laboratories

Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.

Universit£

Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.

Novartis Institutes For Biomedical Research

Selective optimization of side activities: another way for drug discovery.

Prestwick Chemical

Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.

Banyu Tsukuba Research Institute

From hit to lead. Analyzing structure-profile relationships.

Universities Of Lille

Identification and characterization of m1 selective muscarinic receptor antagonists1.

Warner-Lambert

A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.

Warner-Lambert

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

Research Triangle Institute

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

(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.

Virginia Commonwealth University

Identification and characterization of m4 selective muscarinic antagonists.

Parke-Davis Pharmaceutical Research

Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.

Vanderbilt University Medical Center

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

Vanderbilt University Medical Center

Inhalation by design: novel tertiary amine muscarinic M3 receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.

Pfizer

CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.

University Of South Florida

N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.

The University Of Sydney

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

Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.

Pfizer

FRET-based sensors for the human M1-, M3-, and M5-acetylcholine receptors.

University Of Wuerzburg

Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.

The University Of Sydney

Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.

National Institute Of Mental Health

Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators.

Vanderbilt University Medical Center

Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.

Vanderbilt University Medical Center

Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.

Pfizer

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

Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.

University Of Medicine And Dentistry Of New Jersey-Robert Wood Johnson Medical School And The Informatics Institute Of Umdnj

Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template.

Pfizer

 

The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)

TBA

 

The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D₄ (LTD₄)/platelet activating factor (PAF) receptor antagonists.

TBA

 

3-Lithioquinuclidin-2-ene: A novel intermediate for the synthesis of muscarinic agonists and antagonists

TBA

 

New indole derivatives as potent and selective serotonin uptake inhibitors

TBA

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

Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.

Novartis Institutes For Biomedical Research

Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.

Vanderbilt University Medical Center

Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.

Vanderbilt University Medical Center

Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674.

Mitsubishi Pharma

Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata.

Mitsubishi Pharma

Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.

National Institute Of Mental Health

Identification of a novel 4-aminomethylpiperidine class of M3 muscarinic receptor antagonists and structural insight into their M3 selectivity.

Tsukuba Research Institute

An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.

Predix Pharmaceuticals

Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.

Columbia University College Of Physicians And Surgeons

Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.

Columbia University College Of Physicians And Surgeons

Synthesis of potent and selective serotonin 5-HT1B receptor ligands.

Columbia University College Of Physicians And Surgeons

Binding of beta-carbolines at 5-HT(2) serotonin receptors.

Virginia Commonwealth University

C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists.

University Of North Carolina At Chapel Hill

Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists.

The University Of Toledo

Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.

University Of Bologna

Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.

Columbia University College Of Physicians And Surgeons

Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency.

Schering-Plough Research Institute

Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity.

Novo Nordisk

Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.

Royal Danish School Of Pharmacy

A novel class of conformationally restricted heterocyclic muscarinic agonists.

TBA

Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity.

Harvard Medical School

Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.

Yogi Vemana University

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

University Of Washington

Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.

Tehran University Of Medical Sciences

Hydroxybenzaldoximes Are D-GAP-Competitive Inhibitors of E. coli 1-Deoxy-D-Xylulose-5-Phosphate Synthase.

The Johns Hopkins University School Of Medicine

DXP synthase-catalyzed C-N bond formation: nitroso substrate specificity studies guide selective inhibitor design.

The Johns Hopkins University

New insights into the pharmacological chaperone activity of c2-substituted glucoimidazoles for the treatment of Gaucher disease.

Nankai University

Beyond topoisomerase inhibition: antitumor 1,4-naphthoquinones as potential inhibitors of human monoamine oxidase.

Federal University Of Rio De Janeiro