Abstract：
:Three membrane preparations of rat cortex were used to examine the effects of GABA, bicuculline and bicucine on specific 3H-diazepam binding. In the crude synaptosomal fraction, GABA had no effect on either the maximal binding capacity (Bmax) or dissociation constant (KD) of 3H-diazepam binding. Bicuculline and bicucine both decreased binding affinity. This was antagonized by adding GABA. In the repeatedly washed membrane preparation, and in the washed, frozen and thawed preparation, GABA increased binding affinity and, at high concentrations, increased Bmax. Increased binding affinity was observed with as little as 10(-8) M GABA in the washed, frozen and thawed preparation. Bicuculline inhibited the effect of GABA on 3H-diazepam binding. It was found that about 3 X 10(-5) M GABA was present in the assay medium containing crude synaptosomal fraction. These results suggest endogenous GABA is present in, and influences the results of 3H-diazepam binding assays. Furthermore, it appears that GABA and bicuculline affect 3H-diazepam binding through their binding to the specific GABA binding site.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Chiu TH,Rosenberg HCdoi
10.1016/0014-2999(79)90264-4subject
Has Abstractpub_date
1979-07-01 00:00:00pages
337-45issue
4eissn
0014-2999issn
1879-0712pii
0014-2999(79)90264-4journal_volume
56pub_type
杂志文章abstract：:Inhibition of glutamate carboxypeptidase (GCP) II (EC 3.4.17.21), also termed N-acetylated alpha-linked acidic dipeptidase (NAALADase), has been shown to protect against ischemic injury presumably via decreasing glutamate and increasing N-acetyl-aspartyl-glutamate (NAAG). NAAG is a potent and selective mGlu3 receptor ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01239-0
更新日期：2001-10-26 00:00:00
abstract：:The effects of escins Ib and IIb isolated from horse chestnuts on Mg(2+) absorption from the digestive tract and the role of endogenous nitric oxide (NO) were investigated in mice. Test samples were given orally to fasted mice 30, 120, 180, 240 and 300 min before administration of 0.5 M MgSO(4) (10 ml/kg, p.o.). The s...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00772-4
更新日期：2000-01-17 00:00:00
abstract：:The mechanisms underlying the hypothermic effect of ethanol have been investigated in rats. At an ambient temperature of 26 degrees C, at which tail skin blood flow will normally be expected to play a role in regulating core temperature, no change in tail cutaneous temperature occurred during the period in which the c...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90193-x
更新日期：1981-05-22 00:00:00
abstract：:Abnormal proliferation and hypertrophy of vascular smooth muscle (VSMC), as the main structural component of the vasculature, is an important pathological mechanism of hypertension. Recently, increased levels of arginine vasopressin (AVP) and copeptin, the C-terminal fragment of provasopressin, have been shown to corr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.10.023
更新日期：2016-12-05 00:00:00
abstract：:We previously reported that both nitric oxide (NO) generated from NO synthase by bombesin and NO generated from SIN-1 (NO donor) activate the brain cyclooxygenase (COX) (COX-1 for bombesin), thereby eliciting the secretion of both catecholamines (CA) from the adrenal medulla by brain thromboxane A(2)-mediated mechanis...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.01.005
更新日期：2012-03-15 00:00:00
abstract：:Chronic restraint stress (CRS) is known to cause metabolic and neurological complications in a number of ways. Prolonged exposure to stress evident by increased corticosterone level led to impaired altered insulin signaling and oxidative stress in mice, in the present study. Impaired insulin signaling or insulin resis...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.07.056
更新日期：2018-09-15 00:00:00
abstract：:The purpose of this study is to clarify involvement ratios between central and peripheral cyclooxygenase (COX)-2 in rat inflammatory pain models, by evaluating celecoxib and [6-chloro-2-(4-chlorobenzoyl)-1H-indol-3-yl]acetic acid (CIAA) on carrageenan-induced mechanical and thermal hyperalgesia. Celecoxib and CIAA exh...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.07.063
更新日期：2008-01-06 00:00:00
abstract：:CysLT1 receptors are known to be involved in the pathogenesis of asthma. However, the functional roles of CysLT2 receptors in this condition have not been determined. The purpose of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs and use this mod...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.11.036
更新日期：2017-01-05 00:00:00
abstract：:Membrane currents in response to the application of alpha, beta-methylene ATP (alpha,beta-meATP) were recorded by the whole-cell patch-clamp technique in human embryonic kidney 293 cells transfected with the human P2X3 receptor (HEK 293-hP2X3 cells). Trichloroethanol, the biologically active metabolite of chloral hydr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00833-5
更新日期：2000-12-15 00:00:00
abstract：:Epinephrine stimulation of 45Ca2+ efflux and inositol 1,4,5-trisphosphate ((1,4,5)IP3) production in parotid cell aggregates from mature rats was greatly inhibited (approximately 70%) by WB 4101 and 5-methylurapidil as compared to a small decrease by chloroethylclonidine (approximately 30%). The combination of WB 4101...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(92)90173-s
更新日期：1992-06-05 00:00:00
abstract：:Pulmonary hypertension (PH) mainly results from excessive proliferation of pulmonary artery smooth muscle cells (PASMCs) and displays mitochondrial abnormalities such as mitochondrial fragmentation. Epigallocatechin-3-gallate (EGCG), an efficient antiproliferative compound in green tea, has recently been demonstrated ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.05.003
更新日期：2017-08-15 00:00:00
abstract：:The choleretic action of 3-(2,4,5-triethoxybenzoyl)propionic acid (AA-149) was studied in anesthetized dogs. AA-149 produced a dose-dependent increase of the bile flow with both i.v. and intrajejunal administration of doses 1 mg/kg and higher. Biliary clearance of 14C-erythritol showed that AA-149 stimulated canalicul...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90050-x
更新日期：1978-03-01 00:00:00
abstract：:Unlike the situation with the vas deferens of rats, guinea-pigs, rabbits and dogs, neither phentolamine nor yohimbine enhanced electrically-evoked release of [3H]norepinephrine from the in vitro human vas deferens. However, clonidine produced, by a phentolamine-sensitive mechanism, a concentration-related inhibition o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90495-2
更新日期：1982-03-26 00:00:00
abstract：:Receptor autoradiography was used to examine the distribution of muscarinic cholinoceptors ([3H]QNB), alpha 2-adrenoceptors ([3H]rauwolscine), beta-adrenoceptors ([125I]CYP) and substance P receptors ([125I]BHSP) in rabbit aorta, pulmonary artery, rat aorta, dog aorta, splenic, renal and coronary arteries, bovine aort...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90128-2
更新日期：1987-01-28 00:00:00
abstract：:This study examined the pharmacological characteristics of binding sites for the potent K+ channel opener [3H]P1075, as well as the functional effects of P1075 on ionic currents and membrane potential, in ovine choroid plexus (OCP) cells. [3H]P1075 bound to OCP cells with a Kd of 26 +/- 4 nM and a Bmax of 10400 +/- 48...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01617-8
更新日期：1998-03-12 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：:The effect of various concentrations of 4 beta-phorbol dibutyrate, (4-beta PDBu) phorbol myristate acetate (PMA), and 4 beta-phorbol didecanoate (4 beta-PDD) were studied on the guinea-pig parenchymal strip. The order of potency, 4 beta-PDBu greater than PMA greater than 4 beta-PDD, was the inverse of their lipid solu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90407-9
更新日期：1987-09-02 00:00:00
abstract：:The humanized anti-CD52 antibody alemtuzumab is successfully used in the treatment of multiple sclerosis (MS) and is thought to exert most of its therapeutic action by depletion and repopulation of mainly B and T lymphocytes. Although neuroprotective effects of alemtuzumab have been suggested, direct effects of anti-C...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.172923
更新日期：2020-03-15 00:00:00
abstract：:Several structural analogs of mazindol were tested as inhibitors of the uptake of [3H] dopamine in rat neostriatum, of [3H] norepinephrine in rat occipital cortex and of [3H] serotonin in whole rat brain. A rather wide range of potencies was observed but a number of the drugs were even more potent than mazindol as upt...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90030-3
更新日期：1981-05-08 00:00:00
abstract：:The alpha 1-adrenoceptors present in the liver of rhesus monkeys was characterized using [3H]prazosin. This radioligand binds to monkey liver membranes with high affinity (KD 0.33 nM) to a moderately abundant number of sites (97 fmol/mg of protein). These sites were characterized pharmacologically, by binding competit...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00433-5
更新日期：1996-09-12 00:00:00
abstract：:The effect of (+)-sotalol and deoxysotalol on prostaglandin (PGF2a and 15-methyl PGF2alpha)-evoked contractions was studied using the isolated rat uterus. After control responses to prostaglandins had been obtained the uterus was exposed to the nutrient fluid containing 10 microgram/ml of (+)-sotalol, deoxysotalol or ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90138-8
更新日期：1977-11-01 00:00:00
abstract：:Allergic asthma is a chronic disease characterized by early and late asthmatic reactions, airway hyperresponsiveness, airway inflammation and airway remodelling. Changes in l-arginine homeostasis may contribute to all these features of asthma by decreased nitric oxide (NO) production and increased formation of peroxyn...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2008.02.096
更新日期：2008-05-13 00:00:00
abstract：:Ischemic postconditioning (IPO) had been reported as a promising method against myocardial ischemia-reperfusion (I/R) injury, but IPO was later proved with poor clinical benefit. In this study, we compared the protective effects of pinacidil-postconditioning (PPO) and IPO against myocardial I/R injury. Langendorff rat...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.03.027
更新日期：2016-06-05 00:00:00
abstract：:Since orally administered K+ channel openers may have cardiovascular side effects, it is possible that inhaled administration would be preferred for the treatment of asthma. We have investigated whether inhaled levcromakalim and HOE 234 inhibit histamine-induced bronchoconstriction and airway plasma exudation in anaes...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00670-2
更新日期：1996-01-18 00:00:00
abstract：:The displacement of [3H]flunitrazepam by unlabelled flunitrazepam or zolpidem was used to assess the affinity and density of sub-types of GABA(A) receptors in the superior frontal and primary motor cortices of ten alcoholic, seven alcoholic-cirrhotic and ten matched control cases. The binding was best fitted by a mode...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)85422-2
更新日期：1997-05-20 00:00:00
abstract：:We have recently shown that responses to pressor nerve stimulation in the pithed rat are mediated by α(1A)- and α(1D)-adrenoceptors, with no evidence for α(2)-adrenoceptor involvement, and that responses previously identified as α(2)-adrenoceptor mediated are actually α(1D)-adrenoceptor mediated. We have now re-examin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.01.001
更新日期：2012-03-15 00:00:00
abstract：:We have analyzed the effect of quinolizidine alkaloids from Lupinus species upon insulin secretion. Isolated normal rat islets were incubated with 3.3, 8.3, and 16.7 mM glucose, in the presence or absence of different concentrations of lupanine (0.05, 0.5, and 1.0 mM), 13-alpha-OH lupanine, 17-oxo-lupanine, and 2-thio...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.09.008
更新日期：2004-11-03 00:00:00
abstract：:Little research has been conducted investigating the long-term impact of opioid exposure during adolescence. These experiments were conducted to determine the behavioral effects of morphine exposure during periadolescence (postnatal days 30-32) versus young adulthood (postnatal days 65-67) on subsequent sensitivity to...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.10.026
更新日期：2005-12-28 00:00:00
abstract：:WIN 64338 (phosphonium, [[4-[[2-[[bis(cyclohexylamino) methylene] amino]-3-(2-naphthalenyl) 1-oxopropyl]amino]-phenyl]- tributyl, chloride, monohydrochloride) is the first potent nonpeptide competitive bradykinin B2 receptor antagonist as shown in classical pharmacological preparations with no activity in the rabbit a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90017-5
更新日期：1994-12-15 00:00:00
abstract：:Interleukin-8 is assumed to play a central role in the pathogenesis of psoriasis. Since an increased expression of the interleukin-8 receptor has been observed both in polymorphonuclear leukocytes and in affected psoriatic epidermis, we were interested in whether the interleukin-8 receptor could be a molecular target ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90490-1
更新日期：1994-06-13 00:00:00
