• antagonism
  • Compounds possessing "balanced" 5-HT 1A receptor agonism and D 2 antagonism (or weak partial agonism) and, in some cases, combined with other beneficial properties, such as 5-HT 2A receptor antagonism, are efficacious in a broad range of rodent pharmacological models yet have a lower propensity to elicit EPS or metabolic dysfunction. (springer.com)
  • Essentially, samidorphan counteracts any euphoric or pleasurable intoxication derived from buprenorphine that might make it addictive, leaving users with mostly antagonism of the kappa receptor to block the release of "dynorphins" which can improve mood and decrease anxiety. (mentalhealthdaily.com)
  • agonism
  • There is evidence that D1 receptor agonism regulates phospholipase C independent of cAMP, however implications and mechanisms remain poorly understood. (wikipedia.org)
  • We examine data on in vitro binding and agonism and in vivo tests related to (1) positive symptoms (e.g., psychostimulant-induced hyperactivity or prepulse inhibition deficit), (2) negative symptoms (e.g., phencyclidine-induced social interaction deficits and cortical dopamine release), and (3) cognitive deficits (e.g., phencyclidine or scopolamine-induced memory deficits). (springer.com)
  • The buprenorphine facilitates mood enhancement via partial agonism of the mu-opioid receptor (MOR) and full agonism of the kappa opioid receptor (KOR). (mentalhealthdaily.com)
  • ligands
  • The actions of cannabinoids are also regulated by the endocannabinoid system (ECS) which includes enzymes involved in synthesis, uptake and degradation of endogenous cannabinoid ligands, and the CB1 and CB2 receptors. (frontiersin.org)
  • Parkinson's
  • Research interests and ongoing projects include the study of cell replacement and gene therapies for Parkinson's disease, amyotrophic lateral sclerosis, other neurodegenerative diseases, and spinal cord injuries, and the study of plasticity and function of central catecholaminergic systems in primates and humans. (yale.edu)
  • Aged monkeys as a partial model for Parkinson's disease. (yale.edu)
  • serotonin
  • Akimova E, Lanzenberger R, Kasper S (2009) The serotonin-1A receptor in anxiety disorders. (springer.com)
  • who found that a gene-environment interaction (GxE) may explain why life stress is a predictor for depressive episodes in some individuals, but not in others, depending on an allelic variation of the serotonin-transporter-linked promoter region (5-HTTLPR). (wikipedia.org)
  • vitro
  • In the present in vitro electrophysiological studies, we used four different mutant mice, in which the expression of specific DA receptors is either ablated or altered to clarify the involvement of the most abundant DA receptors expressed in the striatum, D1 and D2, in these functions. (jneurosci.org)
  • polymorphisms
  • The D4 receptor gene displays polymorphisms that differ in a variable number tandem repeat present within the coding sequence of exon 3. (wikipedia.org)
  • citation needed] There are slight variations (mutations/polymorphisms) in the human gene: A 48-base pair VNTR in exon 3 C-521T in the promoter 13-base pair deletion of bases 235 to 247 in exon 1 12 base pair repeat in exon 1. (wikipedia.org)
  • Polymorphisms in tryptophan hydroxylase genes were found to be associated with suicidal behavior. (wikipedia.org)
  • psychostimulants
  • In conclusion, dopamine modulation of GABAergic tonic inhibition of D1- and D2-MSNs provides an intrinsic mechanism to differentially affect their excitability in response to psychostimulants and thereby influence their ability to potentiate conditioned reward. (jneurosci.org)
  • rodent
  • Given that these animals do not possess the aberrant neuronal information processing typically associated with schizophrenia, the aim of the current study was to examine the dopamine D2 receptor system in a rodent model of schizophrenia. (aspetjournals.org)
  • AAV2-mediated CLN2 gene transfer to rodent and non-human primate brain results in long-term TPP-I expression compatible with therapy for LINCL. (yale.edu)
  • prolactin
  • We examined whether two semimechanistic models could describe prolactin response in rats and subsequently be translated to predict pituitary dopamine D2 receptor occupancy and plasma prolactin concentrations in humans following administration of paliperidone or remoxipride. (readbyqxmd.com)
  • mediate
  • D2 receptor signaling may mediate protein kinase B, arrestin beta 2, and GSK-3 activity, and inhibition of these proteins results in stunting of the hyperlocomotion in amphetamine treated rats. (wikipedia.org)
  • Lysergic acid diethylamide (LSD) likely interacts with numerous 5-HT receptors to mediate its effects. (pharmacologicalsciences.us)
  • We demonstrate that both dopamine D1- and D2-receptor-expressing MSNs (D-MSNs) additionally harbor extrasynaptic GABA A Rs incorporating α4, β, and δ subunits that mediate tonic inhibition, thereby influencing neuronal excitability. (jneurosci.org)
  • Ropinirole
  • The purpose of this study was to measure dopamine D2/3 receptor occupancy (RO) as a marker of the clinical efficacy of ropinirole in rats via positron emission tomography (PET) using 18F-fallypride as the radiotracer and to explore the relationship between dopamine RO and the plasma concentration of ropinirole via pharmacokinetic-pharmacodynamic modeling. (readbyqxmd.com)
  • D2Sh
  • D2 is encoded by the Dopamine receptor D2 gene (DRD2), of which there are two forms: D2Sh (short) and D2Lh (long): The D2Sh form is pre-synaptically situated, having modulatory functions (viz. (wikipedia.org)
  • Antidepressant
  • Albert PR, Francois BL (2010) Modifying 5-HT1A receptor gene expression as a new target for antidepressant therapy. (springer.com)
  • Although approximately 70% of individuals who receive antidepressant medication derive substantial therapeutic benefit, the remaining 30% are partial or non-responders. (mentalhealthdaily.com)
  • Partial or non-responders to antidepressant medication tend to have poor quality of life, suicidal ideation, and long-term functional impairment. (mentalhealthdaily.com)
  • mice
  • To overcome this issue, in the present study we used four different mutant mice in which the expression of specific DA receptors was ablated. (jneurosci.org)
  • Accordingly, immunohistochemical analyses in both wild-type and D1R-/- mice confirmed the expression of D5 receptors in both cholinergic and parvalbumin-positive interneurons of the striatum. (jneurosci.org)
  • In mice lacking D2 receptors, D2R-/-, the DA-dependent inhibition of GABA transmission was lost in both interneuron populations. (jneurosci.org)
  • We dosed wild-type mice, dopamine 1 receptor knockout mice and dopamine 5 receptor knockout mice undergoing casting-induced disuse atrophy with SKF 81297 to determine if activation of the dopamine 1 and dopamine 5 receptors results in hypertrophy of non-atrophying skeletal muscle and preservation of atrophying skeletal muscle mass and force production. (biomedcentral.com)
  • In dopamine 1 receptor knockout mice, extensor digitorum longus (EDL) and soleus muscle mass and force was not preserved during casting with SKF 81297 treatment, in contrast to significant preservation of casted wild-type mouse EDL and soleus mass and EDL force with SKF 81297 treatment. (biomedcentral.com)
  • Dosing dopamine 5 receptor knockout mice with SKF 81297 did not significantly preserve EDL and soleus muscle mass and force although wild-type mouse EDL mass and force was significantly preserved SKF 81297 treatment. (biomedcentral.com)
  • whereas
  • The D1 and D5 receptors are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4 receptors are members of the D2-like family. (wikipedia.org)
  • It also found that all studies using objective indicators or structured interviews to assess stress replicated the gene-environment interaction fully or partially, whereas all non-replications relied on self-reported measures of adversity. (wikipedia.org)
  • DRD2
  • Some researchers have previously associated the polymorphism Taq 1A (rs1800497) to the DRD2 gene. (wikipedia.org)
  • schizophrenia
  • Mutations in this gene have been associated with various behavioral phenotypes, including autonomic nervous system dysfunction, attention deficit/hyperactivity disorder , schizophrenia and the personality trait of novelty seeking . (wikipedia.org)
  • Val194Gly A polymorphic tandem duplication of 120 bp[citation needed] Mutations in this gene have been associated with various behavioral phenotypes, including autonomic nervous system dysfunction, attention deficit/hyperactivity disorder, schizophrenia and the personality trait of novelty seeking. (wikipedia.org)
  • Although the exact etiology of schizophrenia is not currently known, there is significant evidence for a dysfunction within the mesolimbic dopamine system ( Abi-Dargham, 2004 ). (aspetjournals.org)
  • We investigated whether a single dose of 12 mg blonanserin, which was within the daily clinical dose range (i.e., 8-24 mg) for the treatment of schizophrenia, occupies D3 as well as D2 receptors in healthy subjects. (readbyqxmd.com)
  • isoforms
  • Alternative splicing of this gene results in multiple transcript variants that would encode different isoforms, although some variants may be subject to nonsense-mediated decay (NMD). (wikipedia.org)
  • Alternative splicing of this gene results in three transcript variants encoding different isoforms. (wikipedia.org)
  • Many of GABA's effects are mediated by GABA A receptors (GABA A Rs), which are composed of five subunits drawn from a repertoire of 19 proteins underpinning the expression of multiple receptor isoforms. (jneurosci.org)
  • Thus
  • Thus we hypothesize that activation of the dopamine 1 and/or 5 receptor will increase skeletal muscle cAMP levels thereby modulating skeletal muscle mass and force production. (biomedcentral.com)
  • mutants
  • Vulnerability to acoustic injury was significantly increased in D2, D4 and D5 lines: D1 could not be tested, and no differences were seen in D3 mutants, consistent with a lack of receptor expression. (jneurosci.org)
  • interaction
  • However, it has become clear that not all effects of cannabinoid drugs are attributable to their interaction with CB1 and CB2 receptors. (frontiersin.org)
  • A 2010 review found 17 replications, 8 partial replications (interaction only in females or only with one of several types of adversity), and 9 non-replications (no interaction or an interaction in the opposite direction). (wikipedia.org)
  • compound
  • The invention relates to a method for determining whether a test compound binds preferentially to a membrane receptor R1 or to a membrane receptor R2, these receptors being known to be expressed on the surface of the cells in monomeric, homodimeric or heterodimeric form. (patentsencyclopedia.com)