Keywords: مدولاتور آلوده کننده مثبت; 4HNE; 4-Hydroxy-2-nonenal; AC; Adenylyl cyclase; AD; Alzheimer's disease; AMP; Adenosine monophosphate; AMPK; AMP-activated protein kinase; cAMP; Cyclic adenosine 3â²,5â²-monophosphate; CB; Cannabinoid receptor; CHO; Chinese hamster ovary; DAL; Dehydro-
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Keywords: مدولاتور آلوده کننده مثبت; Jiadifenolide; Bilobalide; Neurotrophic; Neurodegenerative disorders; Convulsions; AMPA; α-amino-3-hydroxy-5-methyl- 4-isoxazolepropionic acid; AP-4; 4-Aminopyridine; CTZ; cyclothiazide; PAM; positive allosteric modulator; PI; protective index; PTZ; pent
Keywords: مدولاتور آلوده کننده مثبت; AC-42; 4-(4-Butyl-1-piperidinyl)-1-(2-methylphenyl)-1-butanone hydrochloride; ACh; acetylcholine; AM; allosteric modulator; BQCA; Benzyl quinolone carboxylic acid; ECL; extracellular loop; FRET; Förster resonance energy transfer; F-V curve; Function -
Keywords: مدولاتور آلوده کننده مثبت; Biased agonism; Positive allosteric modulator; Stimulus bias; Metabotropic glutamate receptor 5; Glutamate (L-glutamic acid PubChem CID: 33032); DHPG (PubChem CID: 108001); VU0424465 (PubChem CID: 53384864); VU0403602 (PubChem CID: 53384878); VU29 (PubChe
Keywords: مدولاتور آلوده کننده مثبت; nAChR; nicotinic acetylcholine receptor; PAM; positive allosteric modulator; cyt c; cytochrome c; CTX; α-cobratoxin; dFBr; desformylflustrabromine hydrochloride; DhβE; dihydro-β-erythroidine; Nicotinic acetylcholine receptor; Mitochondria; Nicotine; Gl
Keywords: مدولاتور آلوده کننده مثبت; Chemokine receptors; CCR5; CCR2; Positive allosteric modulator; 2-Benzazepines; TAK-779; TAK-652; Structure-affinity relationships; Structure activity relationships;
Keywords: مدولاتور آلوده کننده مثبت; Ketamine; Depression; NMDAR; GluN2B; AMPAR; Ambient glutamate; Cortex; Inhibition; Disinhibition; NMDA receptor; AMPA receptor; Homeostatic synaptic plasticity; Protein synthesis; Folimycin (PubChem CID: 6438151); Glutamate (PubChem CID: 33032); Ketamine
Keywords: مدولاتور آلوده کننده مثبت; Traumatic brain injury; Metabotropic glutamate receptor; Neuroprotection; Computer-aided drug design; Positive allosteric modulator
Keywords: مدولاتور آلوده کننده مثبت; BTBR; Black and Tan Brachyury; CB; Cannibinoid; CBT; Cognitive-Behavioural Therapy; CRT; Cognitive Remediation Therapy; DA; dopamine; DLPFC; Dorsolateral Prefrontal Cortex; DSM; Diagnostic and Statistical Manual; EEG; electroencephalography; ERP; Event Re
Keywords: مدولاتور آلوده کننده مثبت; Acetylcholine; Alpha7 nicotinic receptor; Schizophrenia; Positive allosteric modulator; Negative symptoms; Neurocognition;
Keywords: مدولاتور آلوده کننده مثبت; mGluR5; mGlu5; Metabotropic glutamate receptor 5; Schizophrenia; NMDA receptor; Positive allosteric modulator; PAM; Antipsychotic;
Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability
Keywords: مدولاتور آلوده کننده مثبت; mGlu4 PAM; Positive allosteric modulator; CYP induction; Parkinson's disease; Structure-activity relationship;
Coronaridine congeners modulate mitochondrial α3β4* nicotinic acetylcholine receptors with different potency and through distinct intra-mitochondrial pathways
Keywords: مدولاتور آلوده کننده مثبت; Coronaridine congeners; (+)-Catharanthine; (±)-18-Methoxycoronaridine; Mitochondrial nicotinic acetylcholine receptors; Mitochondria-driven apoptosis; α3β4* nicotinic acetylcholine receptors; α3β4-containing nAChRs; NCA; noncompetitive antagonist; WT
Enantiomer-specific positive allosteric modulation of CB1 signaling in autaptic hippocampal neurons
Keywords: مدولاتور آلوده کننده مثبت; DSE; depolarization-induced suppression of excitation; 2-AG; 2-arachidonoyl glycerol; NAM; negative allosteric modulator; PAM; positive allosteric modulator; EPSC; excitatory postsynaptic current; Allosteric; Orthosteric; G protein-coupled receptor; Canna
Neuropeptide oxytocin enhances μ opioid receptor signaling as a positive allosteric modulator
Keywords: مدولاتور آلوده کننده مثبت; Oxytocin; μ opioid receptor; Positive allosteric modulator; Analgesia; G protein-coupled receptor (GPCR);
Positive allosteric modulators of α7* or β2* nicotinic acetylcholine receptors trigger different kinase pathways in mitochondria
Keywords: مدولاتور آلوده کننده مثبت; ACh; acetylcholine; CaKMII; Ca-calmodulin-dependent kinase type II; cyt c; cytochrome c; dFBr; desformylflustrabromine; nAChR; nicotinic acetylcholine receptor; NS-1738; 1-(5-chloro-2-hydroxyphenyl)-3-(2-chloro-5-trifluoromethylphenyl)urea; PAM; positive
Physiological roles of CNS muscarinic receptors gained from knockout mice
Keywords: مدولاتور آلوده کننده مثبت; Cholinergic; Muscarinic; Mice; Knockout; Knock-out; Null mutation; CIN; cholinergic interneuron; CAMKIIα; Ca2+/calmodulin-dependent protein kinase IIα; EPSP; excitatory postsynaptic potentials; HPA; hypothalamic-pituitary-adrenocortical; MAPK; mitogen-a
Electrophysiological investigation of the effect of structurally different bispyridinium non-oxime compounds on human α7-nicotinic acetylcholine receptor activity-An in vitro structure-activity analysis
Keywords: مدولاتور آلوده کننده مثبت; AChE; acetylcholinesterase; ACh; acetylcholine; BP; bispyridinium; CNS; central nervous system; Iâ; iodide; mAChR(s); muscarinic acetylcholine receptor(s); MLA; methyllycaconitine citrate; nAChR(s); nicotinic acetylcholine receptor(s); OP; organophospho
Identification by virtual screening and functional characterisation of novel positive and negative allosteric modulators of the α7 nicotinic acetylcholine receptor
Keywords: مدولاتور آلوده کننده مثبت; Nicotinic acetylcholine receptor; Ion channel; Allosteric modulation; Virtual screening; 5-HT; 5-hydroxytryptamine; DB04763; 1-N-(4-sulfamoylphenethyl)-2,4,6-trimethylpyridinium tetrafluoroborate; AUC; area under the curve; CAII; carbonic anhydrase II; CD
An antidepressant-related pharmacological signature for positive allosteric modulators of α2/3-containing GABAA receptors
Keywords: مدولاتور آلوده کننده مثبت; β-CCT; beta-carboline-3-carboxylate-t-butyl ester; KRM-II-81; 5-(8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole; KRM-II-82; 5-(8-ethynyl-6-phenyl-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole; MP-III-080; 3-ethyl-5-(
In vitro pharmacological characterization of the bispyridinium non-oxime compound MB327 and its 2- and 3-regioisomers
Keywords: مدولاتور آلوده کننده مثبت; CNS; central nervous system; mAChR; muscarinic acetylcholine receptor; MB327; 1,1â²-(propane-1,3-diyl)bis(4-tert-butylpyridinium) di(iodide); nAChR; nicotinic acetylcholine receptor; NMG; N-methylglucamine; OPC(s); organophosphorus compound(s); PAM(s); p
Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M4 PAM VU0467154
Keywords: مدولاتور آلوده کننده مثبت; Positive allosteric modulator; VU0467154; Antipsychotic-like activity; Cognitive enhancement; M4 muscarinic acetylcholine receptor; MK-801; mAChR; muscarinic acetylcholine receptor; PAM; positive allosteric modulator; NMDAR; N-methyl-d-aspartate subtype o
mGlu4 allosteric modulation for treating Parkinson's disease
Keywords: مدولاتور آلوده کننده مثبت; Parkinson's disease; Dyskinesia; Glutamate; Dopamine; mGlu4; 6-OHDA; 6-hydroxydopamine; ADX88178; 4-methyl-N-[5-methyl-4-(1H-pyrazol-4-yl)-1,3-thiazol-2-yl]pyrimidin-2-amine; AIM; abnormal involuntary movements; CODA-RET; complemented donor acceptor reson
Rescue of Fmr1KO phenotypes with mGluR5 inhibitors: MRZ-8456 versus AFQ-056
Keywords: مدولاتور آلوده کننده مثبت; mGluR5; Fmr1; MRZ-8456; AFQ-056; MPEP; Amyloid-beta precursor protein; Aβ; amyloid-beta; ABC-C; Aberrant Behavior Checklist-Community Edition; AGS; audiogenic-induced seizures; APP; amyloid-beta protein precursor; CNS; central nervous system; CTEP; 2-chl
Effects of alpha-7 nicotinic allosteric modulator PNU 120596 on depressive-like behavior after lipopolysaccharide administration in mice
Keywords: مدولاتور آلوده کننده مثبت; Major depression; Nicotinic receptor; Microglia; α7 positive allosteric modulator; Neuroinflammation; Mice; MDD; major depressive disorder; CNS; central nervous system; LPS; lipopolysaccharide; nAChR; nicotinic acetylcholine receptor; PAM; positive allos
Preclinical profile of a dopamine D1 potentiator suggests therapeutic utility in neurological and psychiatric disorders
Keywords: مدولاتور آلوده کننده مثبت; D1 receptor; Dopamine; Eye-blink; Positive allosteric modulator; Potentiator; Parkinson's disease; CREB; cyclic AMP response element binding protein; DETQ; 2-(2,6-dichlorophenyl)-1-((1S,3R)-3-(hydroxymethyl)-5-(2-hydroxypropan-2-yl)-1-methyl-3,4-dihydrois
Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor
Keywords: مدولاتور آلوده کننده مثبت; ACh; acetylcholine; mAChR; muscarinic acetylcholine receptor; GPCR; G protein-coupled receptor; AD; Alzheimer's disease; PAM; positive allosteric modulator; NAM; negative allosteric modulator; TM; transmembrane domain; ECL; extracellular loop; CHO; Chin
Functional properties and mechanism of action of PPTQ, an allosteric agonist and low nanomolar positive allosteric modulator at GABAA receptors
Keywords: مدولاتور آلوده کننده مثبت; Ago-PAM; allosteric agonist and positive allosteric modulator; C/R; concentration-response; ECD; extracellular domain; FMP; FLIPR Membrane Potential Blue; GABA; γ-Aminobutyric acid; GABAAR; GABAA receptor; methaqualone; 2-methyl-3-(o-tolyl)-quinazolin-4(
Synthesis of both enantiomers of 1,2,3,4-tetrahydroisoquinoline derivative IPPAM-1 and enantio-dependency of its positive allosteric modulation of prostacyclin receptor
Keywords: مدولاتور آلوده کننده مثبت; Pulmonary arterial hypertension; Prostacyclin; Prostacyclin receptor; Positive allosteric modulator; Tetrazole derivative;
Structural development of 1,2,3,4-tetrahydroisoquinoline-type positive allosteric modulators of prostacyclin receptor (IPPAMs) to improve metabolic stability, and investigation of metabolic fate
Keywords: مدولاتور آلوده کننده مثبت; Positive allosteric modulator; Metabolic stability; Metabolic fate; CYP P450;
Surface modified nano-lipid drug conjugates of positive allosteric modulators of M1 muscarinic acetylcholine receptor for the treatment of Alzheimer's disease
Keywords: مدولاتور آلوده کننده مثبت; US-FDA; United States Food and Drugs Administration; AD; Alzheimer's disease; ACh; acetylcholine; PAM; positive allosteric modulator; mAChR; muscarinic acetylcholine receptor; AChE; acetylcholine esterase; LDC; lipid drug conjugate; NP; nanoparticle; GP
Integrated regulation of AMPA glutamate receptor phosphorylation in the striatum by dopamine and acetylcholine
Keywords: مدولاتور آلوده کننده مثبت; D1; D2; Muscarinic receptor; S845; Protein kinase A; Caudate putamen; Nucleus accumbens; Positive allosteric modulator; SKF81297 (PubChem CID:1218); (-)-quinpirole hydrochloride (PubChem CID:55397); SCH23390 (PubChem CID:5018); S-(-)-eticlopride hydrochlo
3-Furan-2-yl-N-p-tolyl-acrylamide, a positive allosteric modulator of the α7 nicotinic receptor, reverses schizophrenia-like cognitive and social deficits in rats
Keywords: مدولاتور آلوده کننده مثبت; α7 Nicotinic acetylcholine receptors; Positive allosteric modulator; Animal model of schizophrenia; Cognitive flexibility; Recognition memory; Antipsychotics;
Rho kinase-dependent desensitization of GPR39; a unique mechanism of GPCR downregulation
Keywords: مدولاتور آلوده کننده مثبت; GPR39-C3 (PubChem CID: 091826086); GSB-118 (PubChem CID: 003112012); G-protein-coupled receptor 39; Desensitization; Biased ligand; Positive allosteric modulator; Rho kinase;
B-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor
Keywords: مدولاتور آلوده کننده مثبت; α7 Acetylcholine receptor; Positive allosteric modulator; Allosteric modulation; Schizophrenia; Alzheimer's disease;
Potentiating SLC transporter activity: Emerging drug discovery opportunities
Keywords: مدولاتور آلوده کننده مثبت; SLC; solute carrier; PAM; positive allosteric modulator; SLC1A1; solute carrier family 1 member 1; EAAT1; excitatory amino acid transporter member 1; Gltph; glutamate transporter homolog from Pyrococcus horikoshii; TM; transmembrane; HP; hairpin; smFRET;
A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain
Keywords: مدولاتور آلوده کننده مثبت; NMDA receptor; Positive allosteric modulator; Transmembrane domain; ATD; amino terminal domain; iGluR; ionotropic glutamate receptor; LBD; ligand-binding domain; NAM; negative allosteric modulator; PAM; positive allosteric modulator; TMD; transmembrane do
Mechanism and properties of positive allosteric modulation of N-methyl-d-aspartate receptors by 6-alkyl 2-naphthoic acid derivatives
Keywords: مدولاتور آلوده کننده مثبت; l-glutamate; N-methyl-d-aspartate; Potentiator; Positive allosteric modulator; Deactivation; Ligand-binding domain;
Molecular insights into allosteric modulation of Class C G protein-coupled receptors
Keywords: مدولاتور آلوده کننده مثبت; GABAB; γ-aminobutyric acid receptor B; BMD; bone mass and density; CaSR; calcium-sensing receptor; CHO; Chinese hamster ovary; CRD; cysteine-rich domain; ER; endoplasmic reticulum; Ca2+o; extracellular calcium; pERK1/2; extracellular signal-regulated kin
Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box
Keywords: مدولاتور آلوده کننده مثبت; mGluR5; mGlu5; Positive allosteric modulator; Silent allosteric modulator; Schizophrenia; Cognition;
Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis
Keywords: مدولاتور آلوده کننده مثبت; PFISFKDVNQMIBD-UHFFFAOYSA-N; LTMOLRJYCSLRSB-DFGRBFICSA-N; ADXIKVSKCLYGHD-UHFFFAOYSA-NMetabotropic glutamate receptor; Positive allosteric modulator; mGlu2 PAM; Schizophrenia
Efficacy and safety of an adjunctive mGlu2 receptor positive allosteric modulator to a SSRI/SNRI in anxious depression
Keywords: مدولاتور آلوده کننده مثبت; MDD; major depressive disorder; SSRI; selective serotonin reuptake inhibitor; SNRI; serotonin-norepinephrine reuptake inhibitor; PAM; positive allosteric modulator; mGluR2; metabotropic glutamate 2 receptor; STAR*D; Sequenced Treatment Alternatives to Rel
In vitro and in vivo pharmacological characterization of SSD114, a novel GABAB positive allosteric modulator
Keywords: مدولاتور آلوده کننده مثبت; GABAB receptors; Positive allosteric modulator; GTPγS binding; Baclofen-induced sedation/hypnosis
Positive allosteric modulators of α7 nicotinic acetylcholine receptors affect neither the function of other ligand- and voltage-gated ion channels and acetylcholinesterase, nor β-amyloid content
Keywords: مدولاتور آلوده کننده مثبت; 5-HT; 5-hydroxytryptamine (serotonin); m5-HT3AR; murine serotonin type 3A receptor; AChR; nicotinic acetylcholine receptor; ACh; acetylcholine; NMDAR; N-methyl-D-aspartate receptor; AMPAR; α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor; NI
Increased Metabotropic Glutamate Receptor 5 Signaling Underlies Obsessive-Compulsive Disorder-like Behavioral and Striatal Circuit Abnormalities in Mice
Keywords: مدولاتور آلوده کننده مثبت; Circuit; Constitutive activity; mGluR5; Obsessive-compulsive disorder; Positive allosteric modulator; Striatum;
Anticonvulsant effects of structurally diverse GABAB positive allosteric modulators in the DBA/2J audiogenic seizure test: Comparison to baclofen and utility as a pharmacodynamic screening model
Keywords: مدولاتور آلوده کننده مثبت; GABAB; Positive allosteric modulator; Baclofen; Anticonvulsant; Audiogenic seizure; DBA/2J
The 15q13.3 deletion syndrome: Deficient α7-containing nicotinic acetylcholine receptor-mediated neurotransmission in the pathogenesis of neurodevelopmental disorders
Keywords: مدولاتور آلوده کننده مثبت; 15q13.3 deletion; Autism spectrum disorder; Copy number variation; Positive allosteric modulator; Schizophrenia; α7-Containing nicotinic acetylcholine receptor;
Exploring the positive allosteric modulation of human α7 nicotinic receptors from a single-channel perspective
Keywords: مدولاتور آلوده کننده مثبت; Cys-loop receptors; Nicotinic receptors; Patch-clamp; Single-channel recordings; Positive allosteric modulators; nAChR; nicotinic acetylcholine receptor; ACh; acetylcholine; 5-HT3A; serotonin type 3A receptor; PAM; positive allosteric modulator; PAM-2; 3-
A pharmacological assessment of agonists and modulators at α4β2γ2 and α4β2δ GABAA receptors: The challenge in comparing apples with oranges
Keywords: مدولاتور آلوده کننده مثبت; GABAAR; γ-amino butyric acid receptor type A; DS1 and DS2; Delta selective agents 1 and 2; ECD; extracellular domain; ICL; intracellular loop between TM3 and TM4; PAM; positive allosteric modulator; TMD; transmembrane domain; wt.; wild-type; GABAA recept
Radiosynthesis and in vitro validation of 3H-NS14492 as a novel high affinity alpha7 nicotinic receptor radioligand
Keywords: مدولاتور آلوده کننده مثبت; Bmax; maximum density; 125I-BTX; 125I-α-bungarotoxin; Kd; dissociation constant; Ki; inhibition constant; NSB; non-specific binding; OD; optical density; PAM; positive allosteric modulator; SB; specific binding; TB; total binding; TE; tissue equivalent;