123 articles for thisTarget
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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 muscarinic M(2) subtype antagonistic activity of enantiomeric pairs of 3-demethylhimbacine (3-norhimbacine) and its C(4)-epimer.
Kyorin Pharmaceutical
Synthesis and muscarinic M2 subtype antagonistic activity of unnatural ent-himbacine and an enantiomeric pair of (2'S,6'R)-diepihimbacine.
Kyorin Pharmaceutical
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
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
Universit£
Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists.
Astellas Pharma
1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.
Novo Nordisk
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.
University of Catania
Stereoselective synthesis and biodistribution of potent [11C]-labeled antagonists for positron emission tomography imaging of muscarinic receptors in the airways.
Groningen University Hospital
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.
National Institutes of Health
Resolution and in vitro and initial in vivo evaluation of isomers of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate: a high-affinity ligand for the muscarinic receptor.
Oak Ridge National Laboratory (Ornl)
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
Albany Molecular Research
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
The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.
Medical Research Division of American Cyanamid
Synthesis and structure-activity studies of a series of spirooxazolidine-2,4-diones: 4-oxa analogues of the muscarinic agonist 2-ethyl-8-methyl-2,8-diazaspiro[4.5]decane-1,3-dione.
Institute For Drug Discovery Research
Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues.
Research Triangle Institute
Muscarinic receptor binding profile of para-substituted caramiphen analogues.
Virginia Commonwealth University
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
Istituto De Angeli
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.
Institute of Research
Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists.
Nova Pharmaceutical
Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.
Royal Danish School of Pharmacy
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.
Vanderbilt University Medical Center
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
Synthesis and binding affinity of new muscarinic ligands structurally related to oxotremorine
TBA
Synthesis and biological activity of enantiomers of a conformationally restricted muscarone analog
TBA
Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivity
TBA
Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine.
TBA
Cholinergic agents: 2-oxazolidinone analogues of the acetylcholine-receptor muscarinic agonist pilocarpine
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
Isoxazole ring as a useful scaffold in a search for new therapeutic agents.
Wroclaw University
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
Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification.
Schering-Plough Research Institute
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
Synthesis and binding studies of some epibatidine analogues.
Institute of Pharmacy and Biochemistry
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
Conjugation of Short Peptides to Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Determines M
University of Regensburg
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
University of Camerino
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
Yamanouchi Pharmaceutical
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
Preparation of 18F-labeled muscarinic agonist with M2 selectivity.
National Institutes of Health
Pharmacological properties and predicted binding mode of arylmethylene quinuclidine-like derivatives at the ?3?4 nicotinic acetylcholine receptor (nAChR).
Targacept
Syntheses and biological properties of chiral fluoroalkyl quinuclidinyl benzilates.
National Institutes of Health
Synthesis and pharmacological characterization of O-alkynyloximes of tropinone and N-methylpiperidinone as muscarinic agonists.
National University of Singapore
Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine.
Dr. Karl Thomae
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
Synthesis and pharmacological investigation of the enantiomers of muscarone and allomuscarone.
Istituto Chimico-Farmaceutico Dell'Università
Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors.
Abbott Laboratories
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
University of South Carolina
Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.
Taisho Pharmaceutical
Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors.
The Danish University of Pharmaceutical Sciences
In vitro characterization of [3H]MethoxyPyEP, an mGluR5 selective radioligand.
Merck Research Laboratories
N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.
Pudue Pharma Discovery Research
Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists.
University of Melbourne
The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.
Janssen Research Foundation
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
Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding.
TBA
Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro.
Eli Lilly
Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
University of Arizona
Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence.
H. Lundbeck
Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.
Emory University
Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine.
Eli Lilly
The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299.
Preclinical R & D, Astra Arcus
RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.
Roche Bioscience
PNU-96415E, a potential antipsychotic agent with clozapine-like pharmacological properties.
Pharmacia & Upjohn
Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.
SynthÉLabo Recherche
The interaction of the enantiomers of aceclidine with subtypes of the muscarinic receptor.
University of California
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Janssen Research Foundation
BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex.
Boehringer Ingelheim Italia
Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.
Vrije Universiteit
Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo.
Syntex Discovery Research
In vitro and in vivo pharmacological characterization of N6-cyclopentyl-9-methyladenine (N-0840): a selective, orally active A1 adenosine receptor antagonist.
Whitby Research
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
University of Bologna
Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties.
Dainippon Pharmaceutical
GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.
Glaxo Group Research
Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo.
Yamanouchi Pharmaceutical
Characterization of muscarinic M4 binding sites in rabbit lung, chicken heart, and NG108-15 cells.
Glaxo Group Research
Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity.
Eli Lilly
Sertraline, 1S,4S-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine, a new uptake inhibitor with selectivity for serotonin.
Pfizer
A new inhibitor of norepinephrine uptake devoid of affinity for receptors in rat brain.
Eli Lilly
Antidepressant biochemical profile of the novel bicyclic compound Wy-45,030, an ethyl cyclohexanol derivative.
Wyeth Laboratories
Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers.
Organon International
Effects of remoxipride and some related new substituted salicylamides on rat brain receptors.
Astra LÄKemedel
Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
National Institute of Mental Health
Binding of arylpiperazines to 5-HT3 serotonin receptors: results of a structure-affinity study.
Virginia Commonwealth University
Neurochemical profile of Lu 19-005, a potent inhibitor of uptake of dopamine, noradrenaline, and serotonin.
Lundbeck Ais
Characterization of the striatal M2 muscarinic receptor mediating inhibition of cyclic AMP using selective antagonists: a comparison with the brainstem M2 receptor.
Abbott Laboratories
[125]I-spectramide: a novel benzamide displaying potent and selective effects at the D2 dopamine receptor.
Nida Addiction Research Center
The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action.
Novo Industri
Binding of selective antagonists to four muscarinic receptors (M1 to M4) in rat forebrain.
UniversitÉ
Amplification of the rat M2 muscarinic receptor gene by the polymerase chain reaction: functional expression of the M2 muscarinic receptor.
University of Arizona
N-[3H]methylscopolamine labeling of non-M1, non-M2 muscarinic receptor binding sites in rat brain.
University of California
Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the Na+/H+ exchanger, but indicate a common structure on receptor proteins.
Center For Bio-Pharmaceutical Sciences