SR 57227A is a partial agonist/partial antagonist of 5-HT3 receptor and inhibits subsequent 5-HT- or SR 57227A-induced 5-HT3 receptor current.
Sign Up to like & getrecommendations! Published in 2019 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2018.11.174
Abstract: The serotonin (5-hydroxytryptamine) type 3 (5-HT3) receptors are transmembrane ligand-gated ion channels. Although several 5-HT3 receptor agonists have been used as preclinical tools, SR 57227A is the most commonly used 5-HT3 receptor agonist with the… read more here.
Keywords: agonist partial; partial antagonist; ht3 receptor; receptor ... See more keywords
Pharmacogenomics: Know your GPCR mutations (and target them right)
Sign Up to like & getrecommendations! Published in 2018 at "Nature Reviews Drug Discovery"
DOI: 10.1038/nrd.2018.13
Abstract: cause patients to respond differently to the same medication. Therefore, understanding genetic variation in drug targets can maximize efficacy and reduce side effects. In a new study, a team led by M. Madan Babu present… read more here.
Keywords: variant; efficacy; drug; receptor ... See more keywords
Occupancy of dopamine D2 and D3 receptors by a novel D3 partial agonist BP1.4979: a [11C]-(+)-PHNO PET study in humans
Sign Up to like & getrecommendations! Published in 2018 at "Neuropsychopharmacology"
DOI: 10.1038/s41386-018-0285-4
Abstract: There has been considerable interest in the development of dopamine D3 receptor (DRD3) partial agonists and antagonists for the treatment of substance use disorders. Pre-clinical evidence overwhelmingly supports the use of these drugs, but translation… read more here.
Keywords: novel partial; bp1; bp1 4979; agonist bp1 ... See more keywords
Identification of a Novel, Small Molecule Partial Agonist for the Cyclic AMP Sensor, EPAC1
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-00455-7
Abstract: Screening of a carefully selected library of 5,195 small molecules identified 34 hit compounds that interact with the regulatory cyclic nucleotide-binding domain (CNB) of the cAMP sensor, EPAC1. Two of these hits (I942 and I178)… read more here.
Keywords: agonist; small molecule; partial agonist; sensor epac1 ... See more keywords
2-Linoleoylglycerol Is a Partial Agonist of the Human Cannabinoid Type 1 Receptor that Can Suppress 2-Arachidonolyglycerol and Anandamide Activity.
Sign Up to like & getrecommendations! Published in 2019 at "Cannabis and cannabinoid research"
DOI: 10.1089/can.2019.0030
Abstract: Introduction: The cannabinoid type 1 (CB1) receptor and cannabinoid type 2 (CB2) receptor are widely expressed in the body and anandamide (AEA) and 2-arachidonoylglycerol (2-AG) are their best characterized endogenous ligands. The diacylglycerol lipases (diacylglycerol… read more here.
Keywords: cannabinoid type; cb1 receptor; partial agonist; receptor ... See more keywords
0500 Evaluation of the Human Abuse Potential of Single Oral Doses of V117957, a Novel, Highly Potent and Selective Partial Agonist for Nociceptin/Orphanin-FQ Peptide (NOP) Receptors
Sign Up to like & getrecommendations! Published in 2020 at "Sleep"
DOI: 10.1093/sleep/zsaa056.497
Abstract: The satisfactory safety/tolerability profile of V117957, an investigational NOP receptor partial agonist, has been previously established in ~200 healthy subjects with maximum doses at 30mg following a single oral administration and 10mg once daily for… read more here.
Keywords: abuse potential; v117957 1mg; placebo; partial agonist ... See more keywords
Effect of a retinoid X receptor partial agonist on airway inflammation and hyperresponsiveness in a murine model of asthma
Sign Up to like & getrecommendations! Published in 2017 at "Respiratory Research"
DOI: 10.1186/s12931-017-0507-z
Abstract: BackgroundRetinoid X receptors (RXRs) are members of the nuclear receptor (NR) superfamily that mediate signaling by 9-cis retinoic acid, a vitamin A (retinol) derivative. RXRs play key roles not only as homodimers but also as… read more here.
Keywords: murine model; airway; airway inflammation; partial agonist ... See more keywords
Efficacy of low-dose D2/D3 partial agonist pramipexole on neuroleptic-induced extrapyramidal symptoms and symptoms of schizophrenia: a stage-1 open-label pilot study
Sign Up to like & getrecommendations! Published in 2019 at "Neuropsychiatric Disease and Treatment"
DOI: 10.2147/ndt.s205933
Abstract: Objective Some lines of evidence show that D2/D3 receptor partial agonist pramipexole may be effective in the treatment of extrapyramidal symptoms (EPS) and psychiatric symptoms of schizophrenia. Therefore, we analyzed whether a low dose of… read more here.
Keywords: study; symptoms schizophrenia; partial agonist; low dose ... See more keywords
GLYX-13, a NMDA Receptor Glycine-Site Functional Partial Agonist, Attenuates Cerebral Ischemia Injury In Vivo and Vitro by Differential Modulations of NMDA Receptors Subunit Components at Different Post-Ischemia Stage in Mice
Sign Up to like & getrecommendations! Published in 2017 at "Frontiers in Aging Neuroscience"
DOI: 10.3389/fnagi.2017.00186
Abstract: Excessive activation of NMDA receptors (NMDARs) is implicated in pathological synaptic plasticity also known as post-ischemic long-term potentiation (i-LTP) which was produced by glutamate mediated excitotoxicity after stroke. In the past decades, many NMDARs inhibitors… read more here.
Keywords: glyx; nmda receptors; partial agonist; glycine site ... See more keywords
Effect of Tandospirone, a Partial Agonist of the 5-HT1A Receptor, in a Patient With Chronic Poststroke Emotional Incontinence With Anxiousness.
Sign Up to like & getrecommendations! Published in 2019 at "The primary care companion for CNS disorders"
DOI: 10.4088/pcc.18l02403
Abstract: To cite: Tamura T, Shiwaku H, Jitoku D, et al. Effect of tandospirone, a partial agonist of the 5-HT1A receptor, in a patient with chronic poststroke emotional incontinence with anxiousness. Prim Care Companion CNS Disord.… read more here.
Keywords: poststroke emotional; incontinence anxiousness; partial agonist; emotional incontinence ... See more keywords