Abstract：
:Ohmefentanyl has been shown to be 6300 times more potent than morphine for analgesia. The receptor binding characteristics and distribution of [3H]ohmefentanyl in rat brain sections are presented. [3H]Ohmefentanyl bound with high affinity to opioid receptors in a saturable manner (Kd = 0.95 +/- 0.08 nM, Bmax = 337 +/- 14 fmol/mg protein). We used various currently available specific mu, delta and kappa ligands to show that [3H]ohmefentanyl has a high selectivity for the mu opioid receptor. However, [D-Ala2,MePhe4,Gly-ol5]enkephalin (DAGO) was unable to completely inhibit [3H]ohmefentanyl specific binding, while complete inhibition was observed with fentanyl derivatives and the benzomorphan derivative, ethylketocyclazocine. This remaining 20% DAGO-inaccessible [3H]ohmefentanyl specific binding did not correspond to either mu1, delta or kappa sites. Haloperidol and 1,3-di-o-tolylguanidine were able to inhibit DAGO-inaccessible [3H]ohmefentanyl specific binding, suggesting that [3H]ohmefentanyl might also bind to haloperidol-sensitive sigma sites. The topographical distribution of [3H]ohmefentanyl found by autoradiography was generally similar to that of [3H]DAGO. However, in agreement with the biochemical results, quantitative analysis revealed additional sites in several rat brain regions, the greatest discrepancies with [3H]DAGO distribution being observed in cerebellum, central grey, hippocampal formation and locus coeruleus. Finally, our results suggest that this capacity of binding to both mu and sigma sites is shared by various fentanyl derivatives.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Wang H,Pélaprat D,Roques BP,Vanhove A,Chi ZQ,Rostène Wdoi
10.1016/0014-2999(91)90149-kkeywords:
subject
Has Abstractpub_date
1991-02-14 00:00:00pages
341-50issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(91)90149-Kjournal_volume
193pub_type
杂志文章abstract：:The biological properties of neurotensin (NT) and the chicken peptide [Lys8,Asn9]neurotensin-(8-13) (LANT-6) were compared in 3 in vitro assays: (1) competitive inhibition of [3H]NT binding to rat brain synaptic membranes, (2) relaxation of the rat ileum, and (3) contraction of the guinea-pig ileum. The data show that...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90147-x
更新日期：1984-04-06 00:00:00
abstract：:In rat neocortical slices activation of glutamate metabotropic receptors with glutamate, quisqualate and 1S,3R-ACPD caused a spike-evoked afterdepolarization which replaced the normal afterhyperpolarization. In some neocortical neurons the afterdepolarization reached action potential threshold causing prolonged self-s...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(92)90073-5
更新日期：1992-07-01 00:00:00
abstract：:Racemic baclofen, (-)-baclofen and muscimol depressed all spontaneously firing locus coeruleus neurons tested in a slice preparation. Racemic phaclofen (100 microM; 1 mM) moderately antagonized the effects of racemic baclofen without antagonizing those of muscimol. Bicuculline (10, 30, 100 microM) potently antagonized...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90061-1
更新日期：1988-04-27 00:00:00
abstract：:Anti-tumor activity of bakuchiol, an analogue of resveratrol, was investigated on human lung adenocarcinoma A549 cell line. MTT assay revealed that IC(50) of bakuchiol at 72h was 9.58+/-1.12 micromol/l, much lower than that of resveratrol (33.02+/-2.35 micromol/l). Bakuchiol but not resveratrol elevated intracellular ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.06.025
更新日期：2010-09-25 00:00:00
abstract：:Pulmonary hypertension (PH) is a disease with a developmental origin characterized by obstructive vascular remodelling that is partially due to excessive pulmonary arterial smooth muscle cells (PASMCs) proliferation. Paeonol has important effects on vascular cell proliferation, migration, and inflammation, but researc...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.07.017
更新日期：2018-09-05 00:00:00
abstract：:Methoctramine, a selective M2 alpha muscarinic receptor antagonist, was examined for its ability to inhibit carbachol-induced drinking in the rat. Intracerebroventricularly (i.c.v.) administered methoctramine was devoid of activity up to a dose of 100 nmol/rat, whereas higher doses were toxic under our experimental co...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90213-6
更新日期：1989-04-25 00:00:00
abstract：:Omega-3 polyunsaturated fatty acids have been reported to be associated with favorable changes in the respiratory system. To determine one of the mechanisms for this effect, membrane currents were recorded in guinea-pig tracheal myocytes by using the whole-cell voltage clamp technique. Without EGTA in the patch pipett...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00484-1
更新日期：1998-08-21 00:00:00
abstract：:We investigated sex differences in the motor responses to the full and selective dopamine D1-like receptor agonist, (+/-)-6-chloro-7,8-dihydroxyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrobromide (SKF-81297; 0.3, 3, and 10 mg/kg, s.c.), in non-habituated adult rats. In general, SKF-81297 produced a biphasic ef...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01716-8
更新日期：2002-06-07 00:00:00
abstract：:Although, several effects of glucosamine and its sulfated form (sulfated glucosamine) have been proposed for the suppression of osteoarthritis, their exact mechanisms have not been completely elucidated. This study explains the novel possibility of involvement of sulfated glucosamine in improving cellular antioxidant ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.10.027
更新日期：2008-01-28 00:00:00
abstract：:The composition of final submaxillary saliva and of whole gland homogenates were compared in rats treated with 14 daily doses of guanethidine (20 mg/kg body weight) and in untreated controls after stimulation with pilocarpine (10 mg/kg) or carbamylcholine (50-100 mg/kg). A 44% reduction in the volume of saliva and ele...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90200-x
更新日期：1977-01-21 00:00:00
abstract：:Calcium entry blockers can effectively preserve high-energy phosphates in ischemic heart. However, little is known about the optimal timing of drug therapy. The moment of nisoldipine administration in relation to its protective efficacy during ischemia and reperfusion was studied in rat hearts. Nisoldipine (50 nM), gi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90662-4
更新日期：1985-11-26 00:00:00
abstract：:Gastrins and cholecystokinins contract the isolated taenia coli of the guinea-pig. Porcine CCK-39 produced the greatest contractile response and human gastrin-17 I and -34 the weakest. Pentagastrin had the highest affinity to the receptors and non-sulphated CCK-8 the lowest. The contractions produced by the CCK peptid...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90244-3
更新日期：1983-06-03 00:00:00
abstract：:The detrimental cardio-toxic effect of doxorubicin, an effective chemotherapeutic agent, limited its clinical use. It has been claimed that doxorubicin cardio-toxicity occurs through calcium ions (Ca2+) overload and reactive oxygen species production. Agmatine, an endogenous imidazoline receptor agonist, induce uptake...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.12.022
更新日期：2017-02-05 00:00:00
abstract：:NO plays a key role in the pathological mechanisms of articular diseases. As cytoskeletal proteins are responsible for the polymerization, stabilization, and dynamics of the cytoskeleton network, we investigated whether cytoskeletal proteins are the intracellular pathological targets of NO. We aimed at clarifying whet...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.01.032
更新日期：2018-04-05 00:00:00
abstract：:Local anesthetics bind to dopamine transporters and inhibit dopamine uptake in rodent brain. Additionally, local anesthetics are self-administered in rhesus monkeys. The present study determined binding affinities of cocaine and five local anesthetics at dopamine transporters in rhesus monkey brain, and compared bindi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00967-4
更新日期：1999-02-19 00:00:00
abstract：:The study concerned the effect of arachidonic acid metabolites on the inflammatory reaction in granulation tissue of open wounds in rats. Metabolites or inhibitors were applied in a wound chamber attached to circular, open, full-thickness skin wounds 5 days post-wounding. The adjacent wound served as control. Blood fl...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90454-0
更新日期：1984-01-27 00:00:00
abstract：:Cardiovascular and behavioral responses induced by intravenous administration of the serotonin (5-HT)1A receptor agonist, 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), were studied in conscious normotensive rats either after a single administration, after repeated subcutaneous treatments (1 mg/kg daily for 3 day...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90140-l
更新日期：1991-02-14 00:00:00
abstract：:Recent studies suggested the involvement of the endocannabinoid pathway on insulin secretion in RINm5F cells or rat islets. Animal and clinical studies have reported beneficial effects of the selective cannabinoid 1 receptor antagonist rimonabant on glucose homeostasis. The aim of this study was to investigate the in ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.05.024
更新日期：2009-08-15 00:00:00
abstract：:Poly (ADP-ribose) polymerase (PARP), a nuclear enzyme activated by strand breaks in DNA, plays an important role in the colon injury associated with experimental colitis. The aim of the present study was to examine the effects of 3-aminobenzamide (3-AB), an inhibitor of PARP activity, in the development of acute pancr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.08.008
更新日期：2006-11-07 00:00:00
abstract：:The site of the analgesic action of AD-1211, the less active stereoisomer, and its pharmacological features were investigated. AD-1211, as well as pentazocine and morphine, blocked the reflex hypertension caused by injection of both bradykinin and bradykinin plus PGE1 into the splenic artery of dogs. In the rat or mou...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90722-2
更新日期：1984-11-13 00:00:00
abstract：:Sex and stress hormones coordinate experience and behaviour with physiological regulations. In the brain the sex hormones act to promote the repertoire of affiliative and reproductive behaviours. Stress hormones target in particular brain circuits underlying emotional arousal and cognition. To exert these actions the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2009.10.017
更新日期：2010-01-10 00:00:00
abstract：:cRNA encoding the human IsK protein was injected into Xenopus oocytes and the expressed channels were investigated using the two-microelectrode voltage-clamp method. The novel class III antiarrhythmic NE-10064 (1-[[[5-(4-chlorophenyl)-2-furanyl]methylene]-amino]-3- [4-(4-methyl-1-piperazinyl)-butyl]-2,4-imidazolidined...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90632-7
更新日期：1994-10-13 00:00:00
abstract：:Dinitrosyl iron complexes (DNIC) with glutathione exert a cytotoxic effect on endometrioid tumours in rats with surgically induced experimental endometriosis. Intraperitoneal treatment of rats (Group 1) with DNIC (12.5μmoles/kg, daily, for 12 days), beginning with day 4 after the surgical operation (implantation of tw...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.01.002
更新日期：2014-03-15 00:00:00
abstract：:The treatment of rat thymocytes with 10 microM terfenadine resulted in a significant increase in DNA fragmentation. The DNA fragmentation induced by terfenadine was dependent on its concentration and incubation time. In terfenadine-treated cells, the translocation of phosphatidylserine from the inside of plasma membra...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.05.048
更新日期：2004-08-02 00:00:00
abstract：:The tachykinins substance P, neurokinin A and neurokinin B are involved in many pathophysiological processes. A reverse transcription-polymerase chain reaction (RT-PCR) assay was used to analyse the expression of TAC1 and TAC3, the genes that encode substance P/neurokinin A and neurokinin B, respectively, and the gene...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.05.016
更新日期：2004-06-28 00:00:00
abstract：:Sprague-Dawley rats were trained to discriminate a subcutaneous injection of physostigmine (0.2 mg/kg) from a similar injection of saline in a two-lever, food-reinforced behavior paradigm. The training dose of physostigmine reduced the response rate to about 50% of that in saline sessions. The discriminative stimulus ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90592-4
更新日期：1988-08-09 00:00:00
abstract：:Meperidine has atypical opioid receptor agonist effects and shares some structural features with the phenyltropane (WIN) analogs of cocaine. In combination with 0.1 mg/kg naltrexone, meperidine produced cocaine-like discriminative stimulus effects in monkeys, whereas morphine was inactive. Both cocaine and meperidine ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00696-6
更新日期：1996-02-15 00:00:00
abstract：:The D-1 receptor agonist, SKF 38393 (2 mg/kg s.c.), failed to elicit contralateral turning when administered to drug-naive rats 17 days after unilateral 6-hydroxydopamine (6-OHDA) lesioning of the medial forebrain bundle, while it elicited intense contralateral turning 90 days post-lesioning. On the other hand the D-1...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90296-3
更新日期：1989-03-21 00:00:00
abstract：:Activation of cannabinoid receptor 1 (CB1) inhibits synaptic transmission in hippocampal neurons. The goal of this study was to evaluate the ability of benchmark and emerging synthetic cannabinoids to suppress neuronal activity in vitro using two complementary techniques, Ca(2+) spiking and multi-electrode arrays (MEA...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.05.038
更新日期：2016-09-05 00:00:00
abstract：:Risperidone (R 64 766, 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-pyperidinyl]ethyl )-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one) has superior effects in treating negative symptoms of schizophrenia and causes less extrapyramidal side effects than traditional antipsychotics. In this study, we employed ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00160-0
更新日期：1999-04-16 00:00:00
