• full agonists
  • It has nootropic, anorectic, rewarding and antiparkinsonian effects in animal studies, but its high potency and long duration of action causes D1 receptor downregulation and tachyphylaxis, and unlike other D1 full agonists such as SKF-82,958, it does not produce place preference in animals. (wikipedia.org)
  • Ligands
  • Takasu H, Gardella TJ, Luck MD, et al (1999) Amino-terminal modifications of human parathyroid hormone (PTH) selectively alter phospholipase C signaling via the type 1 PTH receptor: implications for design of signal-specific PTH ligands. (springer.com)
  • Unlike most other D2 receptor ligands, piquindone displays Na2+-dependent binding, a property it shares with tropapride, zetidoline, and metoclopramide. (wikipedia.org)
  • 1996
  • Laugwitz KL, Allgeier A, Offermanns S, et al (1996) The human thyrotropin receptor: a heptahelical receptor capable of stimulating members of all four G protein families. (springer.com)
  • Sagan S, Chassaing G, Pradier L, et al (1996) Tachykinin peptides affect differently the second messenger pathways after binding to CHO-expressed human NK-1 receptors. (springer.com)
  • mGlu
  • LY-404,039 has been shown to modulate glutamatergic activity in the limbic and forebrain areas, where group II mGlu receptors are most densely localized. (wikipedia.org)
  • The specific binding of LY-404,039 to human cloned mGlu receptors has been found to be highest for mGluR2 (Ki = 149 ± 11 nM) and relatively high for mGluR3 (Ki = 92 ± 14 nM). (wikipedia.org)
  • neuronal
  • On the other hand, the preservation of D1-mediated rotational behavior and reduced lateral habenula glucose metabolism in the presence of MK-801 despite attenuation of the effects of the D1 agonist in entopeduncular nucleus and substantia nigra pars reticulata suggests that D1 receptor-regulated neuronal pathways exhibit varying degrees of sensitivity to N-methyl-D-aspartate receptor blockade. (semanticscholar.org)
  • functional
  • In functional studies however, rotigotine behaves as a full agonist of D1, D2, and D3 with similar potencies (EC50). (wikipedia.org)
  • The functional activity of LY-404,039 on mGluR receptors has been further demonstrated by investigating the drug's ability to suppress electrically stimulated excitatory postsynaptic potentials, or EPSPs. (wikipedia.org)
  • clozapine
  • It increases the release of dopamine as well as its metabolites DOPAC and HVA in the prefrontal cortex in a manner similar to the atypical antipsychotic clozapine. (wikipedia.org)
  • assay
  • In this assay, a drug was classed as "dopamine-like" if the vasoldilation it produced was not prevented by β-blocking drugs, and did not occur if the drug was injected into the femoral artery. (wikipedia.org)
  • In an assay based on the increase in heart rate (positive chronotropic response) produced by electrical stimulation of the post-ganglionic fibers of cat cardioaccelerator nerve, an i.v. dose of ~ 15 μg/kg DMDA caused a 50% reduction of the response, compared to an approximately 10% decrease produced by the same dose of dopamine. (wikipedia.org)
  • In the dog, an i.v. dose of 16 μg/kg caused an ~ 80% decrease in heart rate in the same cardioaccelerator nerve assay, compared to an ~ 8% decrease produced by dopamine. (wikipedia.org)
  • Pharmacological
  • In recent years, biased agonists as well as pharmacological chaperones have demonstrated the potential to harness G protein-coupled receptor signaling and trafficking and have collectively opened new possibilities in G protein-coupled receptor drug discovery. (springer.com)
  • Combining pharmacological chaperoning and biased agonism properties into a unique given molecule would be of high therapeutic interest in many human diseases resulting from G protein-coupled receptor mutation and misfolding. (springer.com)
  • Cell-permeable pharmacological chaperones have been successfully challenged to restore plasma membrane localization of the receptor mutants and to rescue their function. (springer.com)
  • Because of its structural relationship to dopamine, DMDA has been the subject of a number of pharmacological investigations. (wikipedia.org)
  • stimulation
  • These findings indicate that D1 and D2 receptor-associated brain mechanisms are differentially influenced by N-methyl-D-aspartate receptor stimulation. (semanticscholar.org)
  • D2-mediated behavioral and cerebral metabolic responses appear to require concurrent N-methyl-D-aspartate receptor stimulation. (semanticscholar.org)
  • LY-404,039 has been shown to act as a potent full agonist at group II mGluRs as demonstrated by its ability to inhibit cyclic adenosine monophosphate, cAMP, formation as a result of stimulation by forskolin. (wikipedia.org)
  • 2002
  • Holloway AC, Qian H, Pipolo L, et al (2002) Side-chain substitutions within angiotensin II reveal different requirements for signaling, internalization, and phosphorylation of type 1A angiotensin receptors. (springer.com)
  • regulate
  • 1 Leptin has a variety of important central and peripheral actions to regulate energy balance and metabolism, fertility, and bone metabolism that are mediated by specific cell surface leptin receptors. (ahajournals.org)
  • anticholinergic
  • It also reduces motion sickness and has antiemetic (Histamine H1 receptors but it does not block the production of histamine) and anticholinergic properties. (wikipedia.org)
  • intracellular
  • In most of the cases, it is associated with inactivating mutations of the renal arginine vasopressin V2 receptor leading to misfolding and intracellular retention of the receptor, causing the inability of patients to concentrate their urine in response to the antidiuretic hormone. (springer.com)
  • Therapeutic
  • These compounds, and particularly small-molecule-biased agonists which only trigger the V2-induced Gs protein-dependent signaling pathway, represent a potential therapeutic treatment of this X-linked genetic pathology. (springer.com)
  • knockout
  • For example, low-density lipoprotein-receptor knockout mice lacking leptin (LDLR −/− ob/ob ) develop more atherosclerotic lesions than LDLR −/− control mice. (ahajournals.org)
  • Drug
  • A-77636 partially substituted for cocaine in animal studies, and has been suggested for use as a possible substitute drug in treating addiction, but it is better known for its use in studying the role of D1 receptors in the brain. (wikipedia.org)
  • treatment
  • is an IL-5-alpha receptor antibody used as add-on maintenance treatment in severe eosinophilic asthma. (medicinescomplete.com)
  • is a human monoclonal antibody that targets the interleukin-6 receptor and is licensed for the treatment of moderate to severe active rheumatoid arthritis. (medicinescomplete.com)
  • Rotigotine (Neupro) is a dopamine agonist of the non-ergoline class of medications indicated for the treatment of Parkinson's disease (PD) and restless legs syndrome (RLS). (wikipedia.org)
  • release
  • alcohol makes dopamine release, yes it does, you're loosened up but at the same time hyped up, usually on harder alcohol. (dr-bob.org)
  • but when it leaves the system, your sedated and GABA more in place, the dopamine release is the first couple hours, when it leaves the system your sedated. (dr-bob.org)