ELECTROPHYSIOLOGICAL EFFECTS OF DERMORPHIN ON LOCUS-CERULEUS NEURONS OF RAT

被引:12
作者
CHIU, TH [1 ]
CHEN, TY [1 ]
HO, CL [1 ]
CHIANG, ST [1 ]
机构
[1] ACAD SINICA,INST BIOL CHEM,TAIPEI 115,TAIWAN
关键词
brain slices; dermorphin; intracellular recording; locus coeruleus;
D O I
10.1016/0028-3908(90)90128-E
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
Intracellular recording was used to study the effects of dermorphin on neurons of the locus coeruleus in the rat, in a totally submerged brain slice preparation. Dermorphin caused the inhibition of spontaneous firing of all neurons of the locus coeruleus tested, with an IC50 of 7 nM. Based on the inhibition of spontaneous firing rate, dermorphin was 16.5 times more potent than morphine. Larger concentrations of dermorphin (30-100 nM) further hyperpolarized the neurons of the locus coeruleus and simultaneously caused a reduction in input resistance. These effects were antagonized by naloxone, with a dissociation equilibrium constant of 0.8 nM. The hyperpolarization of neurons of the locus coeruleus, caused by dermorphin, was reversed at a membrane potential of -112mV in this preparation. Furthermore, this hyperpolarization was blocked by cesium chloride and barium chloride. Thus, these data suggest that dermorphin binds to μ-opioid receptors on the cell membrane of neurons of the locus coeruleus. This leads to opening of the inward-going rectification potassium channels, resulting in the observed hyperpolarization of the membrane. © 1990.
引用
收藏
页码:747 / 755
页数:9
相关论文
共 34 条
[1]   COMMON ALPHA-2-EFFECTOR AND OPIATE EFFECTOR MECHANISMS IN THE LOCUS-COERULEUS - INTRACELLULAR STUDIES IN BRAIN-SLICES [J].
AGHAJANIAN, GK ;
WANG, YY .
NEUROPHARMACOLOGY, 1987, 26 (7B) :793-799
[2]   TOLERANCE OF LOCUS COERULEUS NEURONS TO MORPHINE AND SUPPRESSION OF WITHDRAWAL RESPONSE BY CLONIDINE [J].
AGHAJANIAN, GK .
NATURE, 1978, 276 (5684) :186-188
[3]   PERTUSSIS TOXIN BLOCKS THE OUTWARD CURRENTS EVOKED BY OPIATE AND ALPHA-2-AGONISTS IN LOCUS-COERULEUS NEURONS [J].
AGHAJANIAN, GK ;
WANG, YY .
BRAIN RESEARCH, 1986, 371 (02) :390-394
[4]   SPECIFIC OPIOID BINDING-SITES FOR DERMORPHIN IN RAT-BRAIN - A RADIORECEPTOR ASSAY USING THE TRITIATED HORMONE AS PRIMARY LIGAND [J].
AMICHE, M ;
DELFOUR, A ;
MORGAT, JL ;
ROY, J ;
HOUVET, J ;
NICOLAS, P .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1987, 148 (03) :1432-1439
[5]  
ANDRADE R, 1984, J NEUROSCI, V4, P161
[6]  
ANDRADE R, 1985, J NEUROSCI, V5, P2359
[7]   IONTOPHORETIC APPLICATION OF OPIATES TO LOCUS COERULEUS [J].
BIRD, SJ ;
KUHAR, MJ .
BRAIN RESEARCH, 1977, 122 (03) :523-533
[8]   DERMORPHIN, A NEW PEPTIDE FROM AMPHIBIAN SKIN, INHIBITS THE NOCICEPTIVE THALAMIC NEURONS FIRING RATE EVOKED BY NOXIOUS STIMULI [J].
BRAGA, PC ;
TIENGO, M ;
BIELLA, G ;
DALLOGLIO, G ;
FRASCHINI, F .
NEUROSCIENCE LETTERS, 1984, 52 (1-2) :165-169
[9]   PHARMACOLOGICAL DATA ON DERMORPHINS, A NEW CLASS OF POTENT OPIOID-PEPTIDES FROM AMPHIBIAN SKIN [J].
BROCCARDO, M ;
ERSPAMER, V ;
FALCONIERIERSPAMER, G ;
IMPROTA, G ;
LINARI, G ;
MELCHIORRI, P ;
MONTECUCCHI, PC .
BRITISH JOURNAL OF PHARMACOLOGY, 1981, 73 (03) :625-631
[10]   IMMUNOHISTOCHEMICAL DEMONSTRATION OF A DERMORPHIN-LIKE PEPTIDE IN THE RAT-BRAIN [J].
BUFFA, R ;
SOLCIA, E ;
MAGNONI, E ;
RINDI, G ;
NEGRI, L ;
MELCHIORRI, P .
HISTOCHEMISTRY, 1982, 76 (02) :273-276