Safety, Tolerability, and Pharmacokinetics of Mevidalen (LY3154207), a Centrally Acting Dopamine D1 Receptor‐Positive Allosteric Modulator (D1PAM), in Healthy Subjects
Sign Up to like & getrecommendations! Published in 2020 at "Clinical Pharmacology in Drug Development"
DOI: 10.1002/cpdd.874
Abstract: Activation of the brain dopamine D1 receptor has attracted attention because of its promising role in neuropsychiatric diseases. Although efforts to develop D1 agonists have been challenging, a positive allosteric modulator (PAM), represents an attractive… read more here.
Keywords: allosteric modulator; mevidalen ly3154207; healthy subjects; dopamine receptor ... See more keywords
Safety, Tolerability, and Pharmacokinetics of Multiple Repeated Oral Doses of the α2/3/5‐Subtype Selective GABAA‐Positive Allosteric Modulator PF‐06372865 in Healthy Volunteers
Sign Up to like & getrecommendations! Published in 2021 at "Clinical Pharmacology in Drug Development"
DOI: 10.1002/cpdd.912
Abstract: Multiple‐dose pharmacokinetics (PK) and safety were investigated in this phase 1 study of PF‐06372865, a positive allosteric modulator of α2/3/5 subunit‐containing γ‐aminobutyric acid A receptors (NCT03351751). In 2 cohorts (7‐8 PF‐06372865 and 2 placebo in… read more here.
Keywords: allosteric modulator; oral doses; safety; twice daily ... See more keywords
Muscarinic-3-receptor positive allosteric modulator ASP8302 in patients with underactive bladder. A randomized controlled trial.
Sign Up to like & getrecommendations! Published in 2022 at "Neurourology and urodynamics"
DOI: 10.1002/nau.24931
Abstract: AIM The aim of this study is to evaluate safety and efficacy of ASP8302, a novel positive allosteric modulator for the muscarinic M3 receptor (M3-PAM), in patients with underactive bladder (UAB). METHODS A randomized, double-blind,… read more here.
Keywords: muscarinic receptor; allosteric modulator; placebo; bladder ... See more keywords
Additive effects of mGluR2 positive allosteric modulation, mGluR2 orthosteric stimulation and 5-HT2AR antagonism on dyskinesia and psychosis-like behaviours in the MPTP-lesioned marmoset.
Sign Up to like & getrecommendations! Published in 2021 at "Naunyn-Schmiedeberg's archives of pharmacology"
DOI: 10.1007/s00210-021-02162-7
Abstract: PURPOSE Antagonising serotonin (5-HT) type 2A receptors (5-HT2AR) is an effective strategy to alleviate both dyskinesia and psychosis in Parkinson's disease (PD). We have recently shown that activation of metabotropic glutamate 2 receptors (mGluR2), via… read more here.
Keywords: ht2ar antagonism; emd 281; mglur2; dyskinesia psychosis ... See more keywords
Positive allosteric modulation of the cannabinoid type-1 receptor (CB1R) in periaqueductal gray (PAG) antagonizes anti-nociceptive and cellular effects of a mu-opioid receptor agonist in morphine-withdrawn rats.
Sign Up to like & getrecommendations! Published in 2020 at "Psychopharmacology"
DOI: 10.1007/s00213-020-05650-5
Abstract: Opioid drugs are a first-line treatment for severe acute pain and other chronic pain conditions, but long-term opioid drug use produces opioid-induced hyperalgesia (OIH). Co-administration of cannabinoids with opioid receptor agonists produce anti-nociceptive synergy, but… read more here.
Keywords: opioid receptor; morphine; anti nociceptive; receptor ... See more keywords
Development of 1,3-thiazole analogues of imidazopyridines as potent positive allosteric modulators of GABAA receptors.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103334
Abstract: Structure-activity relationship studies were conducted in the search for 1,3-thiazole isosteric analogs of imidazopyridine drugs (Zolpidem, Alpidem). Three series of novel γ-aminobutyric acid receptor (GABAAR) ligands belonging to imidazo[2,1-b]thiazoles, imidazo[2,1-b][1,3,4]thiadiazoles, and benzo[d]imidazo[2,1-b]thiazoles were synthesized and… read more here.
Keywords: allosteric modulators; development thiazole; development; imidazo thiazoles ... See more keywords
Muscarinic receptor M4 positive allosteric modulators attenuate central effects of cocaine.
Sign Up to like & getrecommendations! Published in 2017 at "Drug and alcohol dependence"
DOI: 10.1016/j.drugalcdep.2017.03.014
Abstract: BACKGROUND Cocaine addiction is a chronic brain disease affecting neurotransmission. Muscarinic cholinergic receptors modulate dopaminergic signaling in the reward system, and muscarinic receptor stimulation can block direct reinforcing effects of cocaine. Here, we tested the… read more here.
Keywords: allosteric modulators; muscarinic receptor; cocaine; effects cocaine ... See more keywords
Vasodilatory effects of a variety of positive allosteric modulators of GABAA receptors on rat thoracic aorta.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of pharmacology"
DOI: 10.1016/j.ejphar.2021.174023
Abstract: Different subtypes of GABAA (gamma-aminobutyric acid A) receptors, through their specific regional and cellular localization, are involved in the manifestation of various functions, both at the central and peripheral levels. We hypothesized that various non-neuronal… read more here.
Keywords: thoracic aorta; allosteric modulators; gabaa receptors; rat thoracic ... See more keywords
Agathadiol, a labdane diterpenoid from juniper berries, is a positive allosteric modulator of CB1R.
Sign Up to like & getrecommendations! Published in 2021 at "Fitoterapia"
DOI: 10.1016/j.fitote.2021.105059
Abstract: The neutral fraction of a juniper (Juniperus communis L.) berries acetone extract could positively modulate the activity of type 1 - cannabinoid receptor (CB1R). Bioactivity-directed fractionation identified the labdane diterpenoid agathadiol (4) as a positive… read more here.
Keywords: allosteric modulator; cb1r; juniper; labdane diterpenoid ... See more keywords
Menthol acts as a positive allosteric modulator on nematode levamisole sensitive nicotinic acetylcholine receptors
Sign Up to like & getrecommendations! Published in 2019 at "International Journal for Parasitology: Drugs and Drug Resistance"
DOI: 10.1016/j.ijpddr.2018.12.005
Abstract: The ongoing and widespread emergence of resistance to the existing anti-nematodal pharmacopeia has made it imperative to develop new anthelminthic agents. Historically, plants have been important sources of therapeutic compounds and offer an alternative to… read more here.
Keywords: menthol acts; acetylcholine receptors; levamisole sensitive; nicotinic acetylcholine ... See more keywords
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
Sign Up to like & getrecommendations! Published in 2017 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2016.10.002
Abstract: &NA; The cognitive impairments and negative symptoms experienced by schizophrenia patients still await effective treatment. Alpha7 nicotinic acetylcholine receptors (&agr;7 nAChRs) have gain considerable attention in this regard. It has been recently proposed that positive… read more here.
Keywords: tolyl acrylamide; furan tolyl; ketamine induced; cognitive impairments ... See more keywords