Abstract：
:The inhibition by various serotonin agonists and antagonists of the binding of 3 nM 3H-d-LSD, 1.7 nM 3H-serotonin and 0.22 nM 3H-spiperone to homogenates of calf hippocampus and frontal cortex was studied. The 50% inhibitory concentration (IC50) for these drugs versus 3H-d-LSD binding had similar values to and correlated with corresponding IC50 values versus 3H-serotonin binding in the hippocampus, suggesting that 3H-LSD and 3H-serotonin label similar sites in this region. In the calf frontal cortex, serotonin revealed a biphasic inhibition against 3H-d-LSD binding and the tryptamines inhibited over a concentration range of 10 000-fold. The IC25 values of various drugs versus 3H-d-LSD binding correlated with the IC50 values versus 3H-serotonin, but did not correlate with the IC50 values versus 3H-spiperone. These data suggest that 3H-d-LSD bound to more than one serotonin site in the calf frontal cortex and that 3H-spiperone bound to a separate serotonergic site. Scatchard analyses of the binding for these three 3H-ligands indicated that in the calf frontal cortex the density of 3H-d-LSD sites was approximately equal to the sum of the densities for 3H-serotonin (S-1 sites) and 3H-spiperone (S-2 sites). Two weeks after serotonin-depleting radiofrequency heat lesions of the midbrain dorsal and median raphe nuclei in rats, both 3H-serotonin and 3H-LSD showed enhanced binding in the hippocampus. These data support previous suggestions that supersensitivity develops specifically in serotonin receptors following afferent denervation.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Seeman P,Westman K,Coscina D,Warsh JJdoi
10.1016/0014-2999(80)90141-7subject
Has Abstractpub_date
1980-08-29 00:00:00pages
179-91issue
2-3eissn
0014-2999issn
1879-0712pii
0014-2999(80)90141-7journal_volume
66pub_type
杂志文章abstract：:Clinical evidence indicates an antiarrhythmic effect of sulfonylureas, which might be blunted by their vascular action. We wanted to investigate the effect of glibenclamide and the new sulfonylthiourea compound 1-[[5-[2-(5-chloro-o-anisamido)ethyl]-2-methoxyphenyl]-sulfonyl]-3 -me thylthiourea (HMR1883) on cardiac ele...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00322-8
更新日期：2000-06-16 00:00:00
abstract：:Vasoactive substances released from aggregating platelets inhibit beta-adrenergic neurotransmission in coronary arteries. Studies were carried out on the effects of two such vasoactive substances on canine coronary arteries, at concentrations equivalent to that released by platelets under physiological conditions. 5-H...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90030-6
更新日期：1987-01-20 00:00:00
abstract：:Inhibition of the p38 mitogen-activated protein kinase (MAP Kinase) pathway reduces acute ischemic injury in vivo, suggesting a direct role for this signaling pathway in a number of neurodegenerative processes. The present study was designed to evaluate further the role of p38 MAP Kinase in acute excitotoxic neuronal ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01890-3
更新日期：2002-06-28 00:00:00
abstract：:D,L-Propranolol given in single doses by gavage or s.c. injection to awake rats, always slowed the heart without affecting blood pressure. Doses of 0.2 mg/100 g injected twice daily lowered systolic pressure after 3 days in DOCA hypertensive but not in normotensive or spontaneously hypertensive rats. When chronic trea...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90038-3
更新日期：1977-06-15 00:00:00
abstract：:In the present study we investigated whether muscarinic receptors in human airway smooth muscle are coupled to phosphoinositide metabolism as a possible transduction mechanism of contraction. Using isolated bronchial smooth muscle preparations, we found that the muscarinic agonist methacholine caused a time- and conce...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90480-9
更新日期：1989-05-19 00:00:00
abstract：:Here we investigated the effect of naloxone-precipitated morphine withdrawal on the release of noradrenaline in hippocampus of the anaesthetised rat. Naloxone (1 mg/kg i.p.) injected 3 and 24 h, but not 3 weeks, after eight daily injections of morphine, induced an immediate increase in hippocampal noradrenaline releas...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90052-6
更新日期：1992-05-14 00:00:00
abstract：:We have previously reported that 15-hydroxyeicosatetraenoic acid (15-HETE), a metabolite of arachidonic acid by 15-lipoxygenase, causes pulmonary vasoconstriction via increasing the intracellular Ca(2+) concentration ([Ca(2+)]i). However, the multiple sources of Ca(2+) that contribute to Ca(2+) elevation during and af...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.10.028
更新日期：2008-12-28 00:00:00
abstract：:Hops (Humulus lupulus L.), a major component of beer, contain potentially neuroactive compounds that made it useful in traditional medicine as a sleeping aid. The present study aims to investigate the individual components in hops acting as allosteric modulators in GABAA receptors and bring further insight into the mo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.172962
更新日期：2020-04-15 00:00:00
abstract：:Endogenous opioid peptides have been demonstrated to regulate luteinizing hormone (LH) secretion in a variety of species. Studies in rodents suggest a role of opioid peptide systems in controlling the timing of the LH surge, which is entrained to the circadian rhythm. The current studies utilize clocinnamox, a novel l...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00341-0
更新日期：1998-07-03 00:00:00
abstract：:We have developed an isolated spinal cord-skin preparation of the newborn rat. The spinal cord together with a piece of skin connected to the cord by the saphenous nerve was isolated from 1- to 4-day-old rats and separately superfused with artificial cerebrospinal fluid in two neighbouring chambers. Potentials were re...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90737-o
更新日期：1992-09-22 00:00:00
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 +/-...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90149-k
更新日期：1991-02-14 00:00:00
abstract：:Intracellular accumulation of calcium is thought to play an integral role in the progression of ischemic injury and cell death. We infused the calcium entry blocker, nitrendipine (1.5 micrograms/kg per min), into cats in order to investigate the importance of extracellular Ca2+ influx during hemorrhagic shock. Nitrend...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90510-7
更新日期：1984-01-13 00:00:00
abstract：:Three non-steroidal antiinflammatory agents were tested for their ability to antagonize bradykinin in the rabbit jugular vein, the dog carotid artery and the guinea pig trachea. The new agents were compared with indomethacin, as well as with [Thi5,8,D-Phe7] bradykinin and [Thi6,9,D-Phe8] kallidin, two B2 receptor anta...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90808-4
更新日期：1988-07-07 00:00:00
abstract：:The present study describes the effect of sertindole, clozapine and haloperidol on the number of spontaneously active dopamine neurons in ventral tegmental area and substantia nigra pars compacta after daily oral treatment for 1, 2 or 3 weeks. In general, daily administration of high dosages (sertindole: 2.8 mumol/kg/...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90468-5
更新日期：1994-03-21 00:00:00
abstract：:Oxygen free radicals have been involved in the pathophysiology of cerebral ischemia, especially after spontaneous or thrombolytic reperfusion. In this study with rats, we have combined a severe focal ischemic insult (2 h) and a prolonged reperfusion time (7 days) to assess the possible sustained neuroprotective effect...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.05.024
更新日期：2004-07-08 00:00:00
abstract：:The effects of the long-term administration of diazepam on the potential difference and short-circuit current of the isolated skin of the toad Pleurodema thaul (P. thaul) were investigated. Diazepam applied in a concentration range of 4.6 x 10(-6) to 5.2 x 10(-5) M decreased both electrical parameters. This response w...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00252-g
更新日期：1995-07-04 00:00:00
abstract：:Exposure of cultured heart muscle cells to noradrenaline led to a decrease in the effects of isoproterenol and prostaglandin E1 on cAMP formation and contraction velocity. However, heterologous desensitization, as measured by prostaglandin E1 stimulation, only occurred at higher noradrenaline concentrations than homol...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90370-6
更新日期：1988-09-01 00:00:00
abstract：:Cancer is the second leading cause of mortality worldwide. Therapeutic approach to cancer is a multi-faceted one, whereby many cellular/enzymatic pathways have been discovered as important drug targets for the treatment of cancer. A major disadvantage of most of the currently available anticancer drugs is their non-se...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.05.011
更新日期：2018-08-05 00:00:00
abstract：:Recent studies have reported elevated expression levels in active rheumatoid arthritis patients of the cluster of differentiation (CD) 147 on CD14(+) peripheral blood monocytes and as a result, CD147 may be a target for the development of a novel rheumatoid arthritis therapy. This report describes the inhibitory effec...
journal_title：European journal of pharmacology
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.ejphar.2012.10.030
更新日期：2013-01-05 00:00:00
abstract：:Anandamide is an endogenous ligand at both the inhibitory cannabinoid CB(1) receptor and the excitatory vanilloid receptor 1 (VR1). The CB(1) receptor and vanilloid VR1 receptor are expressed in about 50% and 40% of dorsal root ganglion neurons, respectively. While all vanilloid VR1 receptor-expressing cells belong to...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0014-2999(01)01309-7
更新日期：2001-10-19 00:00:00
abstract：:The genes encoding the alpha3, alpha5 and beta4 subunits of nicotinic acetylcholine receptors are tightly clustered within the genome. As these three subunits constitute the predominant acetylcholine receptor subtype expressed in the peripheral nervous system, their genomic proximity suggests a regulatory mechanism en...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00884-5
更新日期：2000-03-30 00:00:00
abstract：:Cerebral vascular reactivity to prostaglandin E2 was investigated in newborn pigs using closed cranial windows. Exogenous prostaglandin E2 is a dilator of pial arterioles that elevates cyclic AMP in cortical cerebrospinal fluid. Pial arterioles are less sensitive to prostaglandin E2 than to the prostacyclin receptor a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00113-y
更新日期：1995-05-15 00:00:00
abstract：:P815, a murine mastocytoma cell line, possesses beta-adrenergic binding sites as assessed by using [3H]dihydroalprenolol (antagonist) and [3H]hydroxybenzylisoproterenol (agonist). The number of binding sites per cell was 29 000 for the agonist and 75 000 for the antagonist, as determined by direct binding assays and i...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90717-4
更新日期：1985-01-22 00:00:00
abstract：:We tested the hypothesis that calcium from the sarcoplasmic reticulum contributes to exercise-induced muscle damage. Dantrolene sodium (Dantrium) is a muscle relaxant that affects the flux of calcium over the sarcoplasmic membrane. Rats were treated with dantrolene sodium for a week before a 2 h run on a treadmill. We...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90417-5
更新日期：1990-04-10 00:00:00
abstract：:One of the recognized side effects of gentamicin is ototoxicity. The mechanism underlying the organ specificity of this side effect of gentamicin has not been fully established. In view of the fact that a number of pharmacologic agents are known to form complexes with melanin and melanin is an abundant constituent of ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01793-4
更新日期：2002-06-20 00:00:00
abstract：:The sulfonylurea compounds glisoxepide and glibenclamide inhibit the uptake of bile acids into isolated rat hepatocytes. The Ki values for the inhibition of cholate uptake was 9 microM with glibenclamide and 200 microM with glisoxepide. The inhibition of cholate uptake by both sulfonylureas was noncompetitive. Uptake ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90628-h
更新日期：1992-03-31 00:00:00
abstract：:The electrical activity of three different single, identified, spontaneously firing central neurons was monitored by extracellular microelectrodes. Intravenous cocaine administration (0.25-2 mg/kg) elicited an activation of cerebellar Purkinje neurons (PN) and an inhibition of serotonergic dorsal raphe (DRN) and norad...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90520-0
更新日期：1986-11-12 00:00:00
abstract：:The TxA2 receptor antagonist properties of SQ 27,427 [a cyclohexylcarbinol-7-oxabicyclo(2.2.1)heptenoic acid analog] were studied in vitro both in the human platelet and various isolated smooth muscle preparations. SQ 27,427 was found to be a potent inhibitor of human platelet aggregation induced by arachidonic acid, ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90183-3
更新日期：1984-08-03 00:00:00
abstract：:The mouse and tissues from this species are increasingly used as experimental models because of the wide variety of gene deletions and overexpressions available in this species. Yet, very little is known about normal vascular responses in the mouse. We investigated the vasorelaxant responses on thoracic aortic rings f...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01418-2
更新日期：2001-11-16 00:00:00
abstract：:In the isolated perfused guinea-pig heart low-pH buffer (pH 5), lactic acid (5 mM), capsaicin (10(-7) M) and nicotine (10(-4) M) all evoked a clear-cut release of calcitonin gene-related peptide (CGRP) from sensory nerves. Incubation with the proposed capsaicin receptor antagonist, capsazepine (10(-5) M), significantl...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90792-3
更新日期：1992-10-06 00:00:00
