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Abbreviation : PAMs
Long Form : positive allosteric modulators
No. Year Title Co-occurring Abbreviation
2019 A Clinically Applicable Positive Allosteric Modulator of GABA Receptors Promotes Human beta-Cell Replication and Survival as well as GABA's Ability to Inhibit Inflammatory T Cells. GABAA-Rs
2019 A photoreactive analog of allopregnanolone enables identification of steroid-binding sites in a nicotinic acetylcholine receptor. GABAAR, nAChRs, pLGICs
2019 Allosteric Agonism of alpha7 Nicotinic Acetylcholine Receptors: Receptor Modulation Outside the Orthosteric Site. AA, nAChRs
2019 Allosteric Modulation Mechanism of the mGluR5 Transmembrane Domain. GPCR, mGluR5
2019 An Overview, Advantages and Therapeutic Potential of Nonpeptide Positive Allosteric Modulators of Glucagon-Like Peptide-1 Receptor. DPP-4, GLP-1R
2019 Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865). ---
2019 Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT2C Receptor. 5-HT2CR, CUD
2019 Diazepam is not a direct allosteric modulator of alpha1-adrenoceptors, but modulates receptor signaling by inhibiting phosphodiesterase-4. CNS, GPCRs
2019 Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M1 Positive Allosteric Modulators. PK
10  2019 Discovery, Optimization, and Biological Characterization of 2,3,6-Trisubstituted Pyridine-Containing M4 Positive Allosteric Modulators. SAR
11  2019 Fragment Based Optimization of Metabotropic Glutamate Receptor 2 (mGluR2) Positive Allosteric Modulators in the Absence of Structural Information. FBDD, GE, mGluR2
12  2019 GABAA Receptor Subtypes and the Abuse-Related Effects of Ethanol in Rhesus Monkeys: Experiments with Selective Positive Allosteric Modulators. EtOH, FR
13  2019 Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development. ARs
14  2019 Identifying drugs that bind selectively to intersubunit general anesthetic sites in the alpha1beta3gamma2 GABAAR transmembrane domain. GABAARs
15  2019 Large Intracellular Domain-Dependent Effects of Positive Allosteric Modulators on Glycine Receptors. GLIC, GlyRs, ICD
16  2019 Metabotropic functions of the NMDA receptor and an evolving rationale for exploring NR2A-selective positive allosteric modulators for the treatment of autism spectrum disorder. ASD
17  2019 Molecular interactions of type I and type II positive allosteric modulators with the human alpha7 nicotinic acetylcholine receptor: an in silico study. ECD, nAChR, TMD
18  2019 Positron Emission Tomography (PET) Ligand Development for Ionotropic Glutamate Receptors: Challenges and Opportunities for Radiotracer Targeting N-Methyl-d-aspartate (NMDA), alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA), and Kainate Receptors. AMPA, AMPARs, iGluRs, NMDA, NMDARs, PET
19  2019 Potential of GABAB Receptor Positive Allosteric Modulators in the Treatment of Alcohol Use Disorder. AUD, GABAB
20  2019 Simultaneous activation of muscarinic and GABAB receptors as a bidirectional target for novel antipsychotics. ---
21  2019 Suppressing effect of CMPPE, a new positive allosteric modulator of the GABAB receptor, on alcohol self-administration and reinstatement of alcohol seeking in rats. FR, i.p, PR, sP
22  2019 Targeting mGlu Receptors for Optimization of Antipsychotic Activity and Disease-Modifying Effect in Schizophrenia. mGlu
23  2019 The allosteric dopamine D1 receptor potentiator, DETQ, ameliorates subchronic phencyclidine-induced object recognition memory deficits and enhances cortical acetylcholine efflux in male humanized D1 receptor knock-in mice. D1R, NOR
24  2019 The alpha2,3-selective potentiator of GABAA receptors, KRM-II-81, reduces nociceptive-associated behaviors induced by formalin and spinal nerve ligation in rats. ---
25  2019 The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate. VU0652957
26  2019 The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation. mAChR, NAMs
27  2019 The Trifluoromethyl Group as a Bioisosteric Replacement of the Aliphatic Nitro Group in CB1 Receptor Positive Allosteric Modulators (PAMs). ---
28  2018 alpha7 Nicotinic Acetylcholine Receptor: A Potential Target in Treating Cognitive Decline in Schizophrenia. alpha7nAChR
29  2018 alpha7 Nicotinic receptor-modulating agents reverse the hyperdopaminergic tone in the MAM model of schizophrenia. DA, MAM, VTA
30  2018 Amino acid and peptide prodrugs of diphenylpropanones positive allosteric modulators of alpha7 nicotinic receptors with analgesic activity. nAChRs
31  2018 An antidepressant-related pharmacological signature for positive allosteric modulators of alpha2/3-containing GABAA receptors. ---
32  2018 Assessment of the Molecular Mechanisms of Action of Novel 4-Phenylpyridine-2-One and 6-Phenylpyrimidin-4-One Allosteric Modulators at the M1 Muscarinic Acetylcholine Receptors. ACh, BQCA, CHO
33  2018 Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M4 PAM VU0467154. mAChR, NMDAR
34  2018 Discovery of Selective Cannabinoid CB2 Receptor Agonists by High-Throughput Screening. ECS
35  2018 Diversity of Nicotinic Acetylcholine Receptor Positive Allosteric Modulators Revealed by Mutagenesis and a Revised Structural Model. nAChR
36  2018 Effect of Novel Allosteric Modulators of Metabotropic Glutamate Receptors on Drug Self-administration and Relapse: A Review of Preclinical Studies and Their Clinical Implications. mGluRs, NAMs
37  2018 GABAB receptor positive allosteric modulators with different efficacies affect neuroadaptation to and self-administration of alcohol and cocaine. DA, VTA
38  2018 Identification of Global and Ligand-Specific Calcium Sensing Receptor Activation Mechanisms. CaSR, SARs
39  2018 Identification of Positive Allosteric Modulators of the D1 Dopamine Receptor That Act at Diverse Binding Sites. ---
40  2018 Interactions of Hallucinogens with the Glutamatergic System: Permissive Network Effects Mediated Through Cortical Layer V Pyramidal Neurons. DRL 72-s, EPSCs, Glu, mGlu2, OX2, PFC
41  2018 LY2087101 and dFBr share transmembrane binding sites in the (alpha4)3(beta2)2 Nicotinic Acetylcholine Receptor. dFBr, nAChRs, TM1
42  2018 M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. PFC
43  2018 Metabotropic glutamate receptors as drug targets for the treatment of absence epilepsy. mGlu, SWDs
44  2018 Microinjection of baclofen and CGP7930 into the ventral tegmental area suppresses alcohol self-administration in alcohol-preferring rats. sP, VTA
45  2018 Molecular function of the novel alpha7beta2 nicotinic receptor. ---
46  2018 Opportunities and challenges in drug discovery targeting metabotropic glutamate receptor 4. CNS, mGlu4
47  2018 PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native Systems. ---
48  2018 Pharmacological modulation of the alpha7 nicotinic acetylcholine receptor in a mouse model of mecamylamine-precipitated nicotine withdrawal. nAChR
49  2018 Pharmacology in translation: the preclinical and early clinical profile of the novel alpha2/3 functionally selective GABAA receptor positive allosteric modulator PF-06372865. qEEG, RO
50  2018 Positive Allosteric Modulation as a Potential Therapeutic Strategy in Anti-NMDA Receptor Encephalitis. NMDARE, NMDARE, NMDARs
51  2018 Positive allosteric modulators of alpha7* or beta2* nicotinic acetylcholine receptors trigger different kinase pathways in mitochondria. nAChRs
52  2018 Potent and selective pharmacodynamic synergy between the metabotropic glutamate receptor subtype 2-positive allosteric modulator JNJ-46356479 and levetiracetam in the mouse 6-Hz (44-mA) model. LEV, LTG, mGlu2, VPA
53  2018 Regulatory Role of G Protein-coupled Receptors in Pancreatic Cancer Development and Progression. cAMP, COX
54  2018 Role of beta2/3-specific GABA-A receptor isoforms in the development of hippocampus kindling epileptogenesis. AD, GABA-A
55  2018 Small-Molecule Positive Allosteric Modulators of the beta2-Adrenoceptor Isolated from DNA-Encoded Libraries. beta2-AR, GPCRs
56  2018 Structural Basis for Binding of Allosteric Drug Leads in the Adenosine A1 Receptor. A1AR, ECL2, GaMD
57  2018 Structure-Activity Relationships of Pan-Galphaq/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators. ACh, mAChRs
58  2018 The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core. ---
59  2018 The mGluR5 positive allosteric modulator VU0409551 improves synaptic plasticity and memory of a mouse model of Huntington's disease. HD, mGluR5
60  2018 The role of loops B and C in determining the potentiation of GABAA receptors by midazolam. ---
61  2018 VU6007477, a Novel M1 PAM Based on a Pyrrolo[2,3-b]pyridine Carboxamide Core Devoid of Cholinergic Adverse Events. ---
62  2017 3-Furan-2-yl-N-p-tolyl-acrylamide, a positive allosteric modulator of the alpha7 nicotinic receptor, reverses schizophrenia-like cognitive and social deficits in rats. alpha7 nAChRs, ASST, NORT, SIT
63  2017 A single-channel mechanism for pharmacological potentiation of GluN1/GluN2A NMDA receptors. LBDs, NMDARs
64  2017 ADX71943 and ADX71441, novel positive allosteric modulators of the GABAB receptor with distinct central/peripheral profiles, show efficacy in the monosodium iodoacetate model of chronic osteoarthritis pain in the rat. GABAB
65  2017 Antinociceptive Effects of a Novel alpha2/alpha3-Subtype Selective GABAA Receptor Positive Allosteric Modulator. ---
66  2017 Attenuation of nicotine taking and seeking in rats by the stoichiometry-selective alpha4beta2 nicotinic acetylcholine receptor positive allosteric modulator NS9283. nAChRs
67  2017 Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs. ---
68  2017 Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides. ---
69  2017 Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides. ---
70  2017 Clinically applicable GABA receptor positive allosteric modulators promote ss-cell replication. GABARs
71  2017 Design and Synthesis of gamma- and delta-Lactam M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity. AEs, CV, GI, PAM
72  2017 Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache. PAM, PPE
73  2017 Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia. ---
74  2017 Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs. AEs
75  2017 Diverse modes of NMDA receptor positive allosteric modulation: Mechanisms and consequences. NMDARs
76  2017 Enantiospecific Allosteric Modulation of Cannabinoid 1 Receptor. CB1R, hCB1R
77  2017 First in human trial of a type I positive allosteric modulator of alpha7-nicotinic acetylcholine receptors: Pharmacokinetics, safety, and evidence for neurocognitive effect of AVL-3288. CNS
78  2017 FRET-Based Sensors Unravel Activation and Allosteric Modulation of the GABAB Receptor. GABA
79  2017 GABAB receptor allosteric modulators exhibit pathway-dependent and species-selective activity. GABABR
80  2017 GABABR-Induced EGFR Transactivation Promotes Migration of Human Prostate Cancer Cells. GABABR, GPCRs, RTKs
81  2017 KK-92A, a novel GABAB receptor positive allosteric modulator, attenuates nicotine self-administration and cue-induced nicotine seeking in rats. GABABR
82  2017 M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss. AD, BQCA, BQZ-12, M1 mAChR
83  2017 Mechanism and properties of positive allosteric modulation of N-methyl-d-aspartate receptors by 6-alkyl 2-naphthoic acid derivatives. LBDs, NMDAR, Po
84  2017 Old drugs with new skills: fenoprofen as an allosteric enhancer at melanocortin receptor 3. MC
85  2017 Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology. NHP
86  2017 Potent Prearranged Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor. GLP-1R, GPCR
87  2017 Prediction of consensus binding mode geometries for related chemical series of positive allosteric modulators of adenosine and muscarinic acetylcholine receptors. ---
88  2017 Reprint of Pharmacological and molecular characterization of the positive allosteric modulators of metabotropic glutamate receptor 2. mGlu2
89  2017 Role of mGlu5 Receptors and Inhibitory Neurotransmission in M1 Dependent Muscarinic LTD in the Prefrontal Cortex: Implications in Schizophrenia. mAChR, mGlu, NMDAR, PFC
90  2017 Significance of the nicotinic alpha7 receptor in cognition and antipsychotic-like behavior in the rat. ASST, CAR, EDS, GAL, MLA, nAChRs, RISP, SCH
91  2017 Supporting the Identification of Novel Fragment-Based Positive Allosteric Modulators Using a Supervised Molecular Dynamics Approach: A Retrospective Analysis Considering the Human A2A Adenosine Receptor as a Key Example. NAMs, SDFB, SuMD
92  2017 Surface modified nano-lipid drug conjugates of positive allosteric modulators of M1 muscarinic acetylcholine receptor for the treatment of Alzheimer's disease. ACh, AChE, AD, LDC-NPs
93  2017 Targeting metabotropic glutamate receptors for novel treatments of schizophrenia. mGlu, NAMs, NMDAR
94  2017 The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cells lacking functional GABAB receptors. PKC, TAK1
95  2017 The interaction between alpha 7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator-activated receptor-alpha represents a new antinociceptive signaling pathway in mice. nAChRs, OEA, PEA, PPAR-alpha
96  2017 The Quantitative Characterization of Functional Allosteric Effects. NAMs
97  2016 4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor. BQCA, M1 mAChR
98  2016 7TM X-ray structures for class C GPCRs as new drug-discovery tools. 1. mGluR5. NAMs
99  2016 Allosteric Modulation of Nicotinic Acetylcholine Receptors: The Concept and Therapeutic Trends. nAChRs
100  2016 An Integrated Approach for Screening and Identification of Positive Allosteric Modulators of N-Methyl-D-Aspartate Receptors. HTS, NMDARs