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rdf:type |
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lifeskim:mentions |
umls-concept:C0028351,
umls-concept:C0030685,
umls-concept:C0034693,
umls-concept:C0034721,
umls-concept:C0036751,
umls-concept:C0175173,
umls-concept:C0205464,
umls-concept:C0382336,
umls-concept:C0391871,
umls-concept:C0529964,
umls-concept:C0680255,
umls-concept:C1283071,
umls-concept:C1709059,
umls-concept:C1963578,
umls-concept:C1979963,
umls-concept:C2003903
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pubmed:issue |
1
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pubmed:dateCreated |
2003-1-10
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pubmed:abstractText |
1 The pharmacological profiles of presynaptic nociceptin/orphanin FQ (N/OFQ) peptide receptors (NOP) modulating 5-hydroxytryptamine (5-HT) and noradrenaline (NE) release in the rat neocortex were characterized in a preparation of superfused synaptosomes challenged with 10 mM KCl. 2 N/OFQ concentration-dependently inhibited K(+)-evoked [(3)H]-5-HT and [(3)H]-NE overflow with similar potency (pEC(50) approximately 7.9 and approximately 7.7, respectively) and efficacy (maximal inhibition approximately 40%). 3 N/OFQ (0.1 micro M) inhibition of [(3)H]-5-HT and [(3)H]-NE overflow was antagonized by selective NOP receptor antagonists of peptide ([Nphe(1)]N/OFQ(1-13)NH(2) and UFP-101; 10 and 1 microM, respectively) and non-peptide (J-113397 and JTC-801; both 0.1 microM) nature. Antagonists were routinely applied 3 min before N/OFQ. However, a 21 min pre-application time was necessary for J-113397 and JTC-801 to prevent N/OFQ inhibition of [(3)H]-NE overflow. 4 The NOP receptor ligand [Phe(1)psi(CH(2)-NH)Gly(2)]N/OFQ(1-13)NH(2) ([F/G]N/OFQ(1-13)NH(2); 3 microM) did not affect K(+)-evoked [(3)H]-NE but inhibited K(+)-evoked [(3)H]-5-HT overflow in a UFP-101 sensitive manner. [F/G]N/OFQ(1-13)NH(2) antagonized N/OFQ actions on both neurotransmitters. 5 The time-dependency of JTC-801 action was studied in CHO cells expressing human NOP receptors. N/OFQ inhibited forskolin-stimulated cAMP accumulation and JTC-801, tested at different concentrations (0.1-10 microM) and pre-incubation times (0, 40 and 90 min), antagonized this effect in a time-dependent manner. The Schild-type analysis excluded a competitive type of antagonism. 6 We conclude that presynaptic NO receptors inhibiting 5-HT and NE release in the rat neocortex have similar pharmacological profiles. Nevertheless, they can be differentiated pharmacologically on the basis of responsiveness to [F/G]N/OFQ(1-13)NH(2) and time-dependent sensitivity towards non-peptide antagonists.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-10369464,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-10498842,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-10602690,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-10742280,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-10807682,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-10832612,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-10928317,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-10940356,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-10956188,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-10998536,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-10998550,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-11059801,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-11101358,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-11290428,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-11323113,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-11383716,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-11425589,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-11546835,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-11815367,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-11834628,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-11906488,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-12010780,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-12025962,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-12163351,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-42548,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-7481766,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-7566152,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-7568328,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-8732266,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-8982509,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-9489602,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-9719588,
http://linkedlifedata.com/resource/pubmed/commentcorrection/12522077-9798925
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0007-1188
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pubmed:author |
pubmed-author:BarnesTimothy ATA,
pubmed-author:BeaniLorenzoL,
pubmed-author:BianchiClementinaC,
pubmed-author:Calo'GirolamoG,
pubmed-author:De RisiCarmelaC,
pubmed-author:GuerriniRemoR,
pubmed-author:LambertDavid GDG,
pubmed-author:MartiMatteoM,
pubmed-author:MelaFloraF,
pubmed-author:MorariMicheleM,
pubmed-author:PaganiniFrancescaF,
pubmed-author:StocchiSaraS
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pubmed:issnType |
Print
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pubmed:volume |
138
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
91-8
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:12522077-Humans,
pubmed-meshheading:12522077-Animals,
pubmed-meshheading:12522077-Rats,
pubmed-meshheading:12522077-Potassium Chloride,
pubmed-meshheading:12522077-Serotonin,
pubmed-meshheading:12522077-Male,
pubmed-meshheading:12522077-Norepinephrine,
pubmed-meshheading:12522077-Cricetinae,
pubmed-meshheading:12522077-Dose-Response Relationship, Drug,
pubmed-meshheading:12522077-Rats, Sprague-Dawley,
pubmed-meshheading:12522077-Synaptosomes,
pubmed-meshheading:12522077-Neocortex,
pubmed-meshheading:12522077-Receptors, Opioid,
pubmed-meshheading:12522077-Receptors, Presynaptic,
pubmed-meshheading:12522077-Opioid Peptides
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