Abstract:
:The role of endogenous enkephalins in behavioural control in mice was investigated by i.v. injection of RB 101 (N-[(R,S)-2-benzyl-3[(S)(2-amino-4- methylthio)butyl dithio]-1-oxopropyl]-L-phenylalanine benzyl ester). RB 101 is a recently reported systemically active mixed inhibitor prodrug of the two enzymes which metabolize the enkephalins neutral endopeptidase 24.11 and aminopeptidase N. RB 101 (2.5-10 mg/kg) induced a dose-dependent long-lasting hyperlocomotion and attenuated the conditioned suppression of motility in mice placed in an environment where they had received footshocks 24 h before. In addition, RB 101 decreased the duration of immobility in the forced swim test. All these actions of RB 101 were antagonized by the selective delta antagonist, naltrindole, supporting the preferential involvement of delta opioid receptors in these enkephalin-controlled behavioural responses. The effects induced by RB 101 were also suppressed by prior administration of the selective dopamine D1 antagonist, SCH 23390, but not by the D2 antagonist, sulpiride. Attenuation of the conditioned suppression of motility was associated with increased striatal dihydroxyphenylacetic acid (DOPAC)/dopamine (DA) and homovanillic acid (HVA)/DA ratios, both effects being antagonized by naltrindole. This latter compound is also efficient to inhibit the effect of imipramine in the mouse forced swim test. Taken together, these results support the occurrence of tonic and phasic controls of mood-related behaviour by endogenous enkephalins through delta and D1 receptor stimulation and suggest a possible future use of these mixed inhibitors as new antidepressants.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Baamonde A,Daugé V,Ruiz-Gayo M,Fulga IG,Turcaud S,Fournié-Zaluski MC,Roques BPdoi
10.1016/0014-2999(92)90356-9keywords:
subject
Has Abstractpub_date
1992-06-05 00:00:00pages
157-66issue
2eissn
0014-2999issn
1879-0712pii
0014-2999(92)90356-9journal_volume
216pub_type
杂志文章abstract::Lesions of the nucleus basalis magnocellularis and the medial septal area have been shown to produce both deficits in memory and decreases in choline acetyltransferase levels. In order to determine whether functional changes in acetylcholine receptor sensitivity also occur, the present experiment examined the ability ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90619-x
更新日期:1988-08-24 00:00:00
abstract::The modification of proteins with O-linked N-acetylglucosamine (O-GlcNAc) is increasingly recognized as an important posttranslational modification that modulates cellular function. Recent studies suggested that augmentation of O-GlcNAc levels increase cell survival following stress. Salidroside, one of the active com...
journal_title:European journal of pharmacology
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abstract::In the spinal cord of the pentobarbitone-anaesthetised cat, microelectrophoretic pitrazepin reduced the inhibitory effects on neuronal firing of both glycine and GABA. ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(86)90590-x
更新日期:1986-11-19 00:00:00
abstract::Phenoxybenzamine greatly attenuated phenylephrine-induced contractions of dog saphenous vein in vitro, but had less effect on contractions induced by clonidine. The phenoxybenzamine-resistant responses to clonidine were not affected by prazosin or by corynanthine but were competitively antagonized by yohimbine (pA2 8....
journal_title:European journal of pharmacology
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doi:10.1016/0014-2999(82)90219-9
更新日期:1982-12-03 00:00:00
abstract::With age an increase in prostatic smooth muscle tone mediated by α1L-adrenoceptors contributes to the lower urinary tract symptoms associated with benign prostatic hyperplasia. Current treatments for benign prostatic hyperplasia include α1-adrenoceptor antagonists which inhibit smooth muscle contraction. However, musc...
journal_title:European journal of pharmacology
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abstract::Extravasation elicited in rat skin by antidromic electrical stimulation of the saphenous nerve was dose dependently inhibited by the intravenous (i.v.) application of the mu-opioid receptor agonists, morphine and [D-Ala2,Me-Phe4,Gly-ol5]enkephalin (DAGO), and the kappa-opioid receptor agonists (-)-U 50488H, (-)-ICI 19...
journal_title:European journal of pharmacology
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doi:10.1016/0014-2999(93)90233-8
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abstract::The effects of P2Y receptor agonists on smooth muscle membrane potential in isolated ring segments of rat mesenteric artery were examined by intracellular microelectrodes. In the presence of inhibitors of nitric oxide-synthase and cyclo-oxygenase, the selective P2Y1 receptor agonist adenosine 5'-O-thiodiphosphate (ADP...
journal_title:European journal of pharmacology
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doi:10.1016/s0014-2999(98)00848-6
更新日期:1999-01-08 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90626-4
更新日期:1982-04-23 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.02.062
更新日期:2008-05-31 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90363-8
更新日期:1994-03-11 00:00:00
abstract::In Krebs solution (3.36 mM Ca2+), the maximal contractile response of human ileal and urinary bladder detrusor muscle to acetylcholine (ACh) was 40-60% that to carbachol (CCh). The maximum response to ACh was reached at a bath concentration of about 1 microM and was maintained throughout a range extending to 100 micro...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(86)90698-9
更新日期:1986-04-09 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90254-7
更新日期:1985-01-08 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)01223-7
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abstract::The present studies demonstrate that adenylate cyclase and cyclic 3',5'-adenosine monophosphate (cAMP)-phosphodiesterase activities in dog bronchus are comparable to those found in other smooth muscle preparations. Catecholamines, in the order isoproterenol greater than epinephrine greater than norepinephrine, increas...
journal_title:European journal of pharmacology
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更新日期:1977-01-07 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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更新日期:1994-04-21 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.12.003
更新日期:2013-01-30 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)90737-o
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
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doi:10.1016/0014-2999(86)90234-7
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journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
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abstract::Tracazolate (ICI 136,753) 4-butylamine-1-ethyl-6-methyl-1H-pyrazolo[3,4]pyridine-5-carboxylic acid ethyl ester is a non-benzodiazepine with anxiolytic-like activity in animal models. In contrast to the benzodiazepines, it enhances [3H]flunitrazepam binding in rat synaptic membrane fragments. The enhancement is potenti...
journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00861-6
更新日期:1996-04-04 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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更新日期:2015-10-05 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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更新日期:2002-11-01 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90006-r
更新日期:1990-10-09 00:00:00