PMID

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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

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

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

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

Vanderbilt University Medical Center

 

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

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

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

Solvay Duphar

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

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

Dr. Karl Thomae

Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine.

Niddk

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

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