• receptor
  • Second, a better understanding of the neuronal mechanisms by which DA increases the emergence from anesthesia will also help in the management of patients with DA abnormalities as may be the case for patients with Parkinson disease, schizophrenic patients treated with depot neuroleptics (long-acting dopamine-2 receptor [D2R] antagonists) and drug abusers. (asahq.org)
  • 5 report that the dopamine-1 receptor (D1R) agonist 6-chloro-7,8-dihydroxy-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrobromide but not the D2R agonist quinpirole reduces the time to emergence from isoflurane anesthesia in rats by 85% compared with placebo. (asahq.org)
  • Although the role of protein kinase A (PKA) and dopamine and cyclic adenosine 3′,5′ monophosphate-regulated phosphoprotein 32 kDa in NAcb dopamine receptor throughput has been studied extensively, the contribution of protein kinase C (PKC) to NAcb firing is poorly understood. (jneurosci.org)
  • The aim of this study was to use pharmacological inhibition of protein kinase A and mutation of potential protein kinase A phosphorylation sites to determine the role of protein kinase A-catalyzed phosphorylation of the dopamine D 1 receptor in agonist-stimulated desensitization and internalization of the receptor. (aspetjournals.org)
  • To facilitate purification and imaging of the D 1 receptor, we attached a polyhistidine tag to the amino terminus and enhanced green fluorescent protein to the carboxyl terminus of the receptor (D 1 -EGFP). (aspetjournals.org)
  • D 1 -EGFP was similar to the untagged D 1 receptor in terms of affinity for agonist and antagonist ligands, coupling to G proteins, and stimulation of cyclic AMP accumulation. (aspetjournals.org)
  • Pretreatment with the protein kinase A inhibitor H-89 ( N -[2-( p -bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide) or substitution of Ala for Thr268 reduced agonist-stimulated phosphorylation of the receptor and resulted in diminished trafficking of the receptor to the perinuclear region of the cell. (aspetjournals.org)
  • Substitution of Ala for Ser380 had no effect on D 1 receptor phosphorylation, sequestration, desensitization, or trafficking to the perinuclear region. (aspetjournals.org)
  • We conclude that protein kinase A-dependent phosphorylation of the D 1 receptor on Thr268 regulates a late step in the sorting of the receptor to the perinuclear region of the cell, but that phosphorylation of Thr268 is not required for receptor sequestration or maximal desensitization of cyclic AMP accumulation. (aspetjournals.org)
  • The dopamine D 1 receptor belongs to the superfamily of heptahelical receptors that modulate the activity of effectors such as adenylate cyclase by activation of specific heterotrimeric GTP-binding proteins (G proteins). (aspetjournals.org)
  • The mechanisms of desensitization and resensitization have been perhaps most thoroughly characterized for the β-adrenergic receptor, a Gα s -coupled receptor that is structurally and functionally homologous to the D 1 receptor. (aspetjournals.org)
  • amino
  • Here we show that dopamine-mediated enhancement of spike firing in NAcb shell medium spiny neurons was prevented by the PKC inhibitor bisindolylmaleimide but not by the phospholipase C inhibitor 1-[6-((17b-3-methoxyestra-1,3,5(10)-trien-17-yl) amino)hexyl]-1H-pyrrole-2,5-dione, suggesting a role for a diacylglycerol-independent atypical PKC (aPKC) isoform. (jneurosci.org)
  • For experiments with bisindolylmaleimide and 1-[6-((17b-3-methoxyestra-1,3,5(10)-trien-17-yl) amino)hexyl]-1H-pyrrole-2,5-dione ( U73122 ), slices were pre-exposed for 30-60 min to enable adequate penetration, and whole-cell patch was achieved 10-15 min before dopamine application. (jneurosci.org)
  • findings
  • 5 These new data in the setting of isoflurane anesthesia are intriguing and supplement older data reporting similar findings with phenobarbital anesthesia. (asahq.org)
  • The findings suggest the presence of both D 1 and D 2 DA receptors in rat anococcygeus muscle and that DA also acts on adrenergic receptors to produce a contractile response of this muscle preparation. (pcom.edu)
  • The role of GABA A receptors is further supported by findings that GABA A antagonists can prevent these effects ( Delini-Stula, 1979 ). (aspetjournals.org)
  • regulation
  • Dopaminergic neurotransmission is prominently implicated in emergence from the minimal conscious state, 1 , 2 general anesthesia, 3 and in sleep-wake regulation. (asahq.org)
  • molecular
  • 4 The molecular mechanisms for these effects are still incompletely understood. (asahq.org)
  • First, from a clinical point of view, accurate knowledge of the molecular basis for emergence from general anesthetics with agents for which no specific antagonists exists ( i.e ., inhalational agents) and for other anesthetic regimens could lead to the development of a range of new drugs specifically designed for rapid emergence. (asahq.org)