作者: R. A. North , J. T. Williams , A. Surprenant , M. J. Christie
关键词: δ-opioid receptor 、 Receptor 、 μ-opioid receptor 、 Biophysics 、 Class C GPCR 、 Potassium channel 、 Chemistry 、 Opioid receptor 、 Neurotransmitter receptor 、 GABAB receptor 、 Internal medicine 、 Endocrinology
摘要: Abstract The effects of agonists at mu and delta opioid receptors were compared by measuring membrane currents under voltage clamp from neurons the rat nucleus locus coeruleus guinea pig submucous plexus. In each tissue, appropriate selective agonist (Tyr-D-Ala-Gly-MePhe-Gly-ol for in or Tyr-D-Pen-Gly-Phe-D-Pen plexus) increased conductance an inwardly rectifying potassium strongly hyperpolarized membrane. The properties affected two opioids could not be distinguished. Experiments with intracellular application guanosine 5'-[gamma-thio]triphosphate indicated that a guanine nucleotide-binding regulatory protein was involved coupling between receptor channel, but there no evidence activation either cAMP-dependent kinase C. It is noted number vertebrate neurotransmitter are coupled to channels. associated these channels has similar activated opioids; this family includes following receptors: acetylcholine M2, norepinephrine alpha 2, dopamine D2, 5-hydroxytryptamine 5-HT1, adenosine A1, gamma-aminobutyric acid GABAB, somatostatin. suggested conserved neuronal effector one types mediates several major transmitters. appear unusual both utilize same mechanism.