174 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist.
Johns Hopkins Medical Institutions
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
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£
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).
Vanderbilt University
Discovery of ML326: The first sub-micromolar, selective M5 PAM.
Vanderbilt University Medical Center
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 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
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.
Vanderbilt Institute of Chemical Biology
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
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.
Banyu Tsukuba Research Institute
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
(+/-)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
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.
Dvanderbilt Program In Drug Discovery
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
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
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
Synthesis, Characterization, and Application of Muscarinergic M
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
Identification of a novel 4-aminomethylpiperidine class of M3 muscarinic receptor antagonists and structural insight into their M3 selectivity.
Tsukuba Research Institute
Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease.
Merck
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
Columbia University College of Physicians and Surgeons
Synthesis and characterization of chiral 6-azaspiro[2.5]octanes as potent and selective antagonists of the M
Vanderbilt University Medical Center
Discovery of VU6028418: A Highly Selective and Orally Bioavailable M
Vanderbilt University
Dibenzodiazepinone-type muscarinic receptor antagonists conjugated to basic peptides: Impact of the linker moiety and unnatural amino acids on M
University of Regensburg
Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M
Vanderbilt University School of Medicine
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
Differently fluorescence-labelled dibenzodiazepinone-type muscarinic acetylcholine receptor ligands with high M
University of Regensburg
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
Novel Potent Muscarinic Receptor Antagonists: Investigation on the Nature of Lipophilic Substituents in the 5- and/or 6-Positions of the 1,4-Dioxane Nucleus.
Universit£
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine M
University of Regensburg
Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency.
Schering-Plough Research Institute
Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes.
Vanderbilt University
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Conjugation of Short Peptides to Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Determines M
University of Regensburg
Muscarinic agonist, (±)-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human M
University of Kentucky
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
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.
University of W£Rzburg
Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists.
Astellas Pharma
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.
Royal Danish School of Pharmacy
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
cis-1,3,4,6,7,11b-Hexahydro-2-methyl-7-phenyl-2H-pyrazino[2,1-a] isoquinoline: a new atypical antidepressant.
TBA
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Qbi Covid-19 Research Group (Qcrg)
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.
Universit£
Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists.
Universit£
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
Universit£
Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.
Johannes Gutenberg-University of Mainz
Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors.
Pfizer
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
Discovery of the first low-shift positive allosteric modulators for the muscarinic M1 receptor.
Roche Pharma Research and Early Development
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.
University of Texas At Austin
Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments.
Universit£
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
Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the M
University of Regensburg
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D
Universit£
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.
Vanderbilt University School of Medicine
Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo.
Case Western Reserve University
Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor.
Wyeth Research
Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis.
Mcgill University
Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex.
Case Western Reserve University
SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.
Sanofi-Synthelabo Recherche
Synthesis and in vitro pharmacology of novel heterocyclic muscarinic ligands.
Universit&Aagrove
Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.
Case Western Reserve University
3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro.
Case Western Reserve University
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.
Case Western Reserve University
Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes.
Aventis Pharma
Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist.
University of Arkansas
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.
Case Western Reserve University
In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs.
WestfÄLische Wilhelms-UniversitÄ
Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders.
Novartis Pharma
The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor.
Case Western Reserve University
Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists.
University of Melbourne
Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity.
Banyu Pharmaceutical
ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.
Abbott Laboratories
Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological medium.
Eli Lilly
Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro.
Eli Lilly
Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.
Smithkline Beecham Pharmaceuticals
Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics.
Mayo Foundation
Binding profile of the selective muscarinic receptor antagonist tripitramine.
University of Pisa
Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes.
National Institute of Mental Health
Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
National Institute of Mental Health
Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
National Institute of Neurological Disorders and Stroke