60 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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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
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
Synthesis and characterization of chiral 6-azaspiro[2.5]octanes as potent and selective antagonists of the M
Vanderbilt University Medical Center
Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine.
Ranbaxy Research Laboratories
Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists.
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
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
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
Distinct structural changes in a G protein-coupled receptor caused by different classes of agonist ligands.
Niddk
Synthesis and pharmacological characterization of O-alkynyloximes of tropinone and N-methylpiperidinone as muscarinic agonists.
National University of Singapore
N-Acylhydrazones as drugs.
National Institute For Science and Technology On Innovation On Neglected Diseases (Inct/Idn)
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
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
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
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