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Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 08/2019, Volume 29, Issue 15, pp. 1928 - 1933
Structural modifications of nicotinamide, a form of vitamin B3, gave rise to a series of compounds ( – ) that exhibit activities as type I positive allosteric... 
Nicotinamide | Positive allosteric modulators | Alzheimer’s disease | α7 nAChR | Cognitive impairment
Journal Article
by Li, X and Xie, WJ and Wang, XT and Huang, ZZ and Bian, XL and Wang, KW and Sun, Q
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, 08/2019, Volume 29, Issue 15, pp. 1928 - 1933
Structural modifications of nicotinamide, a form of vitamin B3, gave rise to a series of compounds (8aa-8ce) that exhibit activities as type I positive... 
APOPTOSIS | alpha 7 nAChR | CHEMISTRY, MEDICINAL | Positive allosteric modulators | PHARMACOLOGICAL CHARACTERIZATION | CHEMISTRY, ORGANIC | RELEASE | IDENTIFICATION | ACETYLCHOLINE-RECEPTOR AGONIST | Nicotinamide | Alzheimer's disease | Cognitive impairment | SUBUNIT
Journal Article
Biological Psychiatry, ISSN 0006-3223, 2015, Volume 78, Issue 7, pp. 463 - 473
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 07/2019, Volume 29, Issue 14, pp. 1714 - 1718
This letter describes progress towards an M PAM preclinical candidate that resulted in the discovery of VU6005806/AZN-00016130. While the thieno[2,3-... 
Structure-activity relationship (SAR) | Pharmacokinetics | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 02/2019, Volume 164, pp. 499 - 516
Allosteric modulators of G-protein-coupled receptors have lately gained significant traction in drug discovery. Recent studies have shown that allosteric... 
Anti-obesity | Serotonin | Negative allosteric modulator | Food intake | Positive allosteric modulator | 5-HT2C receptor | 5-HT2B receptor | DESIGN | CHEMISTRY, MEDICINAL | AGONISTS | DISCOVERY | (2-PHENYLCYCLOPROPYL)METHYLAMINES | POTENT | INHIBITORS
Journal Article
BBA - General Subjects, ISSN 0304-4165, 03/2014, Volume 1840, Issue 3, pp. 1194 - 1203
Among adenosine receptors (ARs) the A subtype exhibits low affinity for the endogenous agonist compared with the A , A , and A subtypes and is therefore... 
1-Benzyl-3-ketoindole derivatives | Positive allosteric modulators | GPCR allosteric modulators | A2B adenosine receptor | Negative allosteric modulators | Ligand–receptor interaction | adenosine receptor | Ligand-receptor interaction
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 02/2019, pp. 499 - 516
Allosteric modulators of G-protein-coupled receptors have lately gained significant traction in drug discovery. Recent studies have shown that allosteric... 
receptor | Anti-obesity | Negative allosteric modulator | Serotonin | Food intake | Positive allosteric modulator | 5-HT
Journal Article
Neuropharmacology, ISSN 0028-3908, 07/2017, Volume 121, pp. 204 - 218
Journal Article
JOURNAL OF BIOLOGICAL CHEMISTRY, ISSN 0021-9258, 08/2019, Volume 294, Issue 32, pp. 12132 - 12145
Nicotinic acetylcholine receptor (nAChR) ligands that lack agonist activity but enhance activation in the presence of an agonist are called positive allosteric... 
nicotinic acetylcholine receptors (nAChR) | ACTIVATION | DOMAIN | MECHANISM | drug design | DOCKING | DESENSITIZATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | ALPHA-5 | allosteric regulation | SOFTWARE | molecular docking | receptor desensitization | positive allosteric modulator | AGONIST | SUBUNIT | Index Medicus
Journal Article
EUROPEAN JOURNAL OF PHARMACOLOGY, ISSN 0014-2999, 07/2016, Volume 783, pp. 85 - 91
Evidence indicates that microglial activation contributes to the pathophysiology and maintenance of neuroinflammatory pain involving central nervous system... 
NICOTINIC ACH RECEPTORS | TACTILE ALLODYNIA | RANDOMIZED CONTROLLED-TRIAL | Microglia | Neuroinflammatory pain | NEUROPATHIC PAIN | THERAPEUTIC TARGETS | PHARMACOLOGY & PHARMACY | Mice | SPINAL-CORD-INJURY | INFLAMMATORY PAIN | RAT HIPPOCAMPUS | TNF-ALPHA | Alpha-7 positive allosteric modulator | Nicotinic receptor | Hippocampus | POSTOPERATIVE PAIN
Journal Article
Journal Article
JOURNAL OF PHARMACOLOGICAL SCIENCES, ISSN 1347-8613, 05/2018, Volume 137, Issue 1, pp. 67 - 75
Oxytocin (OT) is a 9-amine neuropeptide that plays an essential role in mammalian labor, lactation, maternal bonding, and social affiliation. OT has been... 
ACTIVATION | Oxytocin | mu opioid receptor | INVOLVEMENT | RATS | DISORDERS | ASTROGLIAL CELLS | KNOCKOUT MICE | Analgesia | PAIN | NUCLEUS | G protein-coupled receptor (GPCR) | NEURONS | Positive allosteric modulator | PHARMACOLOGY & PHARMACY | INDUCED ANTINOCICEPTION
Journal Article
Cell Calcium, ISSN 0143-4160, 03/2019, Volume 78, pp. 26 - 34
The non-selective second messenger-gated cation channel TRPC6 (transient receptor potential canonical 6) is activated by diacylglycerols (DAG) in a... 
Compound library screening | Patch clamp electrophysiology | Positive allosteric modulator | Calcium ion influx | Transient receptor potential channel | Platelets | ACID | TRPA1 | LIGHT | HYPERFORIN | CELL BIOLOGY | PROTON ACTIVATION | GENE | MUTATION | BINDING | AGONIST | Physiological aspects | Protein kinases
Journal Article