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1. Full Text Pharmacology and therapeutics of bronchodilators
by Cazzola, Mario and Page, Clive P and Calzetta, Luigino and Matera, M. Gabriella
Pharmacological Reviews, ISSN 0031-6997, 2012, Volume 64, Issue 3, pp. 450 - 504
Bronchodilators are central in the treatment of of airways disorders. They are the mainstay of the current management of chronic obstructive pulmonary disease... 
BETA-ADRENOCEPTOR AGONISTS | RANDOMIZED CONTROLLED-TRIALS | OBSTRUCTIVE PULMONARY-DISEASE | METHACHOLINE-INDUCED BRONCHOCONSTRICTION | LONG-ACTING BETA-AGONISTS | ATRIAL-NATRIURETIC-PEPTIDE | INHALED BETA-ADRENOCEPTOR AGONIST | EXERCISE-INDUCED BRONCHOCONSTRICTION | PHARMACOLOGY & PHARMACY | AIRWAY SMOOTH-MUSCLE | GUINEA-PIG TRACHEA | Bronchodilator Agents - therapeutic use | Asthma - metabolism | Xanthines - adverse effects | Humans | Muscarinic Antagonists - adverse effects | Adrenergic beta-Agonists - pharmacology | Bronchodilator Agents - pharmacology | Muscarinic Antagonists - therapeutic use | Xanthines - therapeutic use | Xanthines - pharmacology | Asthma - drug therapy | Drug Discovery | Asthma - genetics | Animals | Muscarinic Antagonists - pharmacology | Adrenergic beta-Agonists - therapeutic use | Pulmonary Disease, Chronic Obstructive - metabolism | Bronchodilator Agents - adverse effects | Adrenergic beta-Agonists - adverse effects | Drug Combinations | Pulmonary Disease, Chronic Obstructive - drug therapy | Pulmonary Disease, Chronic Obstructive - genetics
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2. Full Text "Phenotypic" pharmacology: The influence of cellular environment on G protein-coupled receptor antagonist and inverse agonist pharmacology
by Nelson, Carl P and Challiss, R.A. John
Biochemical Pharmacology, ISSN 0006-2952, 03/2007, Volume 73, Issue 6, pp. 737 - 751
A central dogma of G protein-coupled receptor (GPCR) pharmacology has been the concept that unlike agonists, antagonist ligands display equivalent affinities... 
G protein-coupled receptor | Receptor dimerization | Signal transduction | Antagonism | Cell background | Muscarinic receptor | Receptor phosphorylation | Adrenoceptor | Inverse agonism | adrenoceptor | antagonism | signal transduction | ALPHA-ADRENOCEPTOR SUBTYPES | SOLIFENACIN SUCCINATE YM905 | CONSTITUTIVE ACTIVITY | receptor phosphorylation | cell background | SB 216469 ROLE | muscarinic receptor | ISOLATED URINARY-BLADDER | VASCULAR SMOOTH-MUSCLE | MUSCARINIC ACETYLCHOLINE-RECEPTOR | ALPHA-1L ADRENOCEPTOR | receptor dimerization | IN-VITRO | SMALL MESENTERIC-ARTERY | PHARMACOLOGY & PHARMACY | inverse agonism | Receptors, Adrenergic, beta - chemistry | Alternative Splicing | RNA Editing | Humans | Male | Adrenergic alpha-Antagonists - pharmacology | Adrenergic Antagonists - pharmacology | Phenotype | Animals | Signal Transduction - drug effects | Muscarinic Antagonists - pharmacology | Receptors, G-Protein-Coupled - antagonists & inhibitors | Receptors, Adrenergic, beta - classification | Polymorphism, Single Nucleotide | Receptors, G-Protein-Coupled - genetics | Receptors, G-Protein-Coupled - drug effects | Prostatic Hyperplasia - drug therapy | Receptors, G-Protein-Coupled - chemistry
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3. Full Text Selective Muscarinic Receptor Agonist Xanomeline as a Novel Treatment Approach for Schizophrenia
by Shekhar, Anantha and Potter, William Z and Lightfoot, Jeffrey and Lienemann, John and Dubé, Sanjay and Mallinckrodt, Craig and Bymaster, Frank P and McKinzie, David L and Felder, Christian C
American Journal of Psychiatry, ISSN 0002-953X, 08/2008, Volume 165, Issue 8, pp. 1033 - 1039
Objective: There are significant unmet needs in the treatment of schizophrenia, especially for the treatment of cognitive impairment, negative syndrome, and... 
SYSTEM | PSYCHIATRY | PHARMACOLOGY | ENHANCEMENT | RISPERIDONE | OLANZAPINE | RATING-SCALE | BINDING | Demography | Muscarinic Agonists - pharmacology | Humans | Middle Aged | Muscarinic Agonists - therapeutic use | Male | Affect | Thiadiazoles - adverse effects | Pyridines - adverse effects | Receptors, Muscarinic - drug effects | Muscarinic Agonists - adverse effects | Thiadiazoles - therapeutic use | Adult | Female | Pyridines - therapeutic use | Thiadiazoles - pharmacology | Severity of Illness Index | Double-Blind Method | Receptors, Cholinergic - drug effects | Schizophrenia - epidemiology | Neuropsychological Tests | Cognition Disorders - diagnosis | Brief Psychiatric Rating Scale | Adolescent | Pyridines - pharmacology | Schizophrenia - drug therapy | Cognition Disorders - epidemiology | Schizophrenia | Research | Drug therapy | Muscarinic receptors | Health aspects | Agonists (Biochemistry) | Psychotropic drugs | Drugs | Birth control | Side effects | Parkinsons disease | Information processing | Alzheimers disease | Clinical outcomes | Chronic illnesses | Dementia | Index Medicus | Abridged Index Medicus
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4. Full Text Structure-Based Design and Discovery of New M-2 Receptor Agonists
by Fish, I and Stossel, A and Eitel, K and Valant, C and Albold, S and Huebner, H and Moller, D and Clark, MJ and Sunahara, RK and Christopoulos, A and Shoichet, BK and Gmeiner, P
JOURNAL OF MEDICINAL CHEMISTRY, ISSN 0022-2623, 11/2017, Volume 60, Issue 22, pp. 9239 - 9250
Muscarinic receptor agonists are characterized by apparently strict restraints on their tertiary or quaternary amine and their distance to an ester or related... 
ENERGY | CHEMISTRY, MEDICINAL | DATABASE | PHARMACOLOGY | CHARGES | MODEL | INHIBITOR | EXPRESSION | MUSCARINIC ACETYLCHOLINE-RECEPTORS | ZINC | Receptor, Muscarinic M2 - agonists | Cricetulus | Muscarinic Agonists - pharmacology | Humans | Benzofurans - pharmacology | Tritium | Acetylcholine - metabolism | Receptor, Muscarinic M3 - chemistry | Quaternary Ammonium Compounds - chemistry | Receptor, Muscarinic M2 - chemistry | Muscarinic Agonists - chemical synthesis | Benzofurans - chemistry | Receptor, Muscarinic M1 - agonists | Receptor, Muscarinic M1 - chemistry | Receptors, Nicotinic - chemistry | Drug Design | HEK293 Cells | Arrestin - metabolism | CHO Cells | Receptor, Muscarinic M2 - metabolism | Receptor, Muscarinic M3 - metabolism | Benzofurans - chemical synthesis | Isoxazoles - pharmacology | Carbachol - pharmacology | Animals | Ligands | Molecular Docking Simulation | Muscarinic Agonists - chemistry | N-Methylscopolamine - chemistry | Quaternary Ammonium Compounds - chemical synthesis | Receptor, Muscarinic M3 - agonists | Receptor, Muscarinic M1 - metabolism | Quaternary Ammonium Compounds - pharmacology
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5. Full Text Electrophysiological evidence showing muscarinic agonist-antagonist activities of N -DESMETHYLCLOZAPINE USING hIPpOCAMPAL EXCITATORY aND INHIBITORY nEURONS
by Sugawara, Yuto and Kikuchi, Yui and Yoneda, Mitsugu and Ohno-Shosaku, Takako
Brain Research, ISSN 0006-8993, 2016, Volume 1642, pp. 255 - 262
Abstract The atypical antipsychotic clozapine is widely used for treatment-resistant schizophrenic patients. Clozapine and its major active metabolite,... 
Neurology | K+channel | N-desmethylclozapine | Muscarinic antagonist | Clozapine | Muscarinic agonist | Hippocampus | Abbreviations oxo-M oxotremorine M | EPSC excitatory postsynaptic current | IPSC inhibitory postsynaptic current | PLC phospholipase C | TTX tetrodotoxin | NDMC N-desmethylclozapine | NMDA N-methyl-d-aspartate | ACTIVATION | POSSIBLE INVOLVEMENT | NEUROSCIENCES | K+ channel | TRANSMISSION | SENSORIMOTOR GATING FUNCTION | ANTIPSYCHOTICS | PYRAMIDAL CELLS | PHARMACOLOGY | RECEPTORS | MODULATION | Oxotremorine - pharmacology | Muscarinic Agonists - pharmacology | Rats | Clozapine - analogs & derivatives | Hippocampus - drug effects | Receptor, Muscarinic M1 - physiology | Rats, Sprague-Dawley | Clozapine - pharmacology | Animals | Muscarinic Antagonists - pharmacology | Oxotremorine - analogs & derivatives | Neurons - physiology | Antipsychotic Agents - pharmacology | Hippocampus - physiology | Neurons - drug effects | Schizophrenia | Neurons | Methyl aspartate | Metabolites
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6. Full Text Model-based Drug Development
by Lalonde, R L and Kowalski, K G and Hutmacher, M M and Ewy, W and Nichols, D J and Milligan, P A and Corrigan, B W and Lockwood, P A and Marshall, S A and Benincosa, L J and Tensfeldt, T G and Parivar, K and Amantea, M and Glue, P and Koide, H and Miller, R
Clinical Pharmacology & Therapeutics, ISSN 0009-9236, 07/2007, Volume 82, Issue 1, pp. 21 - 32
The low productivity and escalating costs of drug development have been well documented over the past several years. Less than 10% of new compounds that enter... 
TRIPTANS SEROTONIN | METAANALYSIS | PAIN | DOSE-RESPONSE | INTEGRATION | 5-HT1B/1D AGONISTS | CLINICAL-TRIALS | DISEASE | PHARMACOLOGY & PHARMACY | SIMULATION | MIGRAINE | Analgesics - pharmacology | Muscarinic Agonists - pharmacology | Cholesterol - blood | Humans | Glycoproteins - pharmacology | Caproates - therapeutic use | Amines - therapeutic use | Alzheimer Disease - psychology | Neutrophil Infiltration - drug effects | United States Food and Drug Administration | Glycoproteins - therapeutic use | Alzheimer Disease - drug therapy | gamma-Aminobutyric Acid - pharmacology | Stroke - drug therapy | Cognition - drug effects | Bridged Bicyclo Compounds, Heterocyclic - pharmacology | Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacology | Models, Biological | Hydroxymethylglutaryl-CoA Reductase Inhibitors - therapeutic use | Amines - pharmacology | Immunologic Factors - pharmacology | Clinical Trials as Topic - legislation & jurisprudence | Guidelines as Topic | Meta-Analysis as Topic | Clinical Trials as Topic - statistics & numerical data | United States | Caproates - pharmacology | Muscarinic Agonists - therapeutic use | Oximes - therapeutic use | Drug Approval | Hypercholesterolemia - drug therapy | Dose-Response Relationship, Drug | Bridged Bicyclo Compounds, Heterocyclic - therapeutic use | Computer Simulation | Drug Design | gamma-Aminobutyric Acid - therapeutic use | Stroke - immunology | Analgesics - therapeutic use | Cyclohexanecarboxylic Acids - therapeutic use | Hypercholesterolemia - blood | Reproducibility of Results | Neuralgia, Postherpetic - drug therapy | Pharmacology | Models, Statistical | Animals | Anticholesteremic Agents - therapeutic use | Cyclohexanecarboxylic Acids - pharmacology | Oximes - pharmacology | Clinical Trials as Topic - methods | Pharmacokinetics | Research Design | Anticholesteremic Agents - pharmacology | Immunologic Factors - therapeutic use
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7. Full Text Exploring the Mechanism of Agonist Efficacy: A Relationship between Efficacy and Agonist Dissociation Rate at the Muscarinic M3 Receptor
by David A. Sykes and Mark R. Dowling and Steven J. Charlton
Molecular Pharmacology, ISSN 0026-895X, 09/2009, Volume 76, Issue 3, pp. 543 - 551
Although there are several empirical approaches that enable the comparison of relative agonist efficacy, the molecular basis that underlies differences in the... 
Binding, Competitive | N-Methylscopolamine - pharmacology | Oxotremorine - pharmacology | Cricetinae | Cricetulus | Acetylcholine - pharmacology | Muscarinic Agonists - pharmacology | Humans | Receptor, Muscarinic M3 - metabolism | Acetylcholine - metabolism | Oxotremorine - metabolism | Animals | Models, Biological | Muscarinic Agonists - metabolism | N-Methylscopolamine - metabolism | Kinetics | Receptor, Muscarinic M3 - agonists | CHO Cells
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8. Full Text Agonists with supraphysiological efficacy at the muscarinic M2 ACh receptor
by Schrage, R and Seemann, WK and Klöckner, J and Dallanoce, C and Racké, K and Kostenis, E and De Amici, M and Holzgrabe, U and Mohr, K
British Journal of Pharmacology, ISSN 0007-1188, 05/2013, Volume 169, Issue 2, pp. 357 - 370
Background and Purpose Artificial agonists may have higher efficacy for receptor activation than the physiological agonist. Until now, such superagonism' has... 
label‐free technologies | muscarinic | iperoxo | receptors | dynamic mass redistribution | ACh | cell signalling | Superagonism | GPCR | biased agonism | efficacy | label-free technologies | muscarinic ACh receptors | GPCRs | CELLS | ALLOSTERIC MODULATORS | PROTEIN-COUPLED RECEPTORS | DEPENDENCE | OXOTREMORINE | ACETYLCHOLINE-RECEPTORS | CYCLIC-AMP | M-2 | LIGANDS | FUNCTIONAL SELECTIVITY | PHARMACOLOGY & PHARMACY | Cell Line | Receptor, Muscarinic M2 - agonists | Cricetulus | Receptor, Muscarinic M2 - metabolism | Receptors, G-Protein-Coupled - metabolism | Acetylcholine - pharmacology | Muscarinic Agonists - pharmacology | Humans | Lung - cytology | Isoxazoles - pharmacology | Animals | Signal Transduction - drug effects | Fibroblasts - drug effects | Lung - drug effects | Lung - metabolism | CHO Cells | Fibroblasts - metabolism | GTP-Binding Proteins - metabolism | Quaternary Ammonium Compounds - pharmacology | Heterocyclic compounds | Acetylcholine | Index Medicus | Research Papers with Commentaries
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9. Full Text Muscarinic acetylcholine receptors: mutant mice provide new insights for drug development
by Eglen, Richard M and Wess, Jürgen and Gautam, Dinesh
Nature Reviews Drug Discovery, ISSN 1474-1776, 09/2007, Volume 6, Issue 9, pp. 721 - 733
Muscarinic acetylcholine receptors ( mAChRs), M-1-M-5, regulate the activity of numerous fundamental central and peripheral functions. The lack of small-... 
KNOCK-OUT MICE | SMOOTH-MUSCLE | HIPPOCAMPAL PLASTICITY | INDUCED CONTRACTIONS | BIOTECHNOLOGY & APPLIED MICROBIOLOGY | ALZHEIMERS-DISEASE | N-DESMETHYLCLOZAPINE | TREATMENT STRATEGIES | PHARMACOLOGY & PHARMACY | CENTRAL-NERVOUS-SYSTEM | DEFICIENT MICE | ISOLATED RAT SKIN | Muscarinic Agonists - pharmacology | Muscarinic Agonists - therapeutic use | Receptors, Muscarinic - metabolism | Muscarinic Antagonists - therapeutic use | Muscarinic Antagonists - chemistry | Mice, Knockout | Animals | Muscarinic Antagonists - pharmacology | Drug Design | Ligands | Mice | Muscarinic Agonists - chemistry | Disease Models, Animal | Receptors, Muscarinic - genetics | Receptors, Muscarinic - physiology | Care and treatment | Nervous system | Neural transmission | Degeneration | Regulation | Research | Muscarinic receptors
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10. Full Text Effects of Mirabegron, a Novel β3-Adrenoceptor Agonist, on Primary Bladder Afferent Activity and Bladder Microcontractions in Rats Compared With the Effects of Oxybutynin
by Aizawa, Naoki and Homma, Yukio and Igawa, Yasuhiko
European Urology, ISSN 0302-2838, 2012, Volume 62, Issue 6, pp. 1165 - 1173
Abstract Background Mirabegron is the first β3-adrenoceptor agonist that is clinically effective for overactive bladder. Objective The effects of mirabegron on... 
Urology | Sprague-Dawley rats | Urinary bladder | Afferent | β3-Adrenoceptor | Neurons, Afferent - drug effects | Acetanilides - pharmacology | Rats | Adrenergic beta-3 Receptor Agonists - pharmacology | Neurons, Afferent - physiology | Rats, Sprague-Dawley | Urinary Bladder - innervation | Mandelic Acids - pharmacology | Animals | Muscarinic Antagonists - pharmacology | Muscle Contraction - drug effects | Muscle Contraction - physiology | Female | Urinary Bladder - drug effects | Thiazoles - pharmacology | Urinary Bladder - physiology
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