Abstract:
:Synaptosomal membranes from cat cerebral cortex were labelled with [3H]-quinuclidinyl benzylate ([3H]QNB). There was shown to be a single type of binding site with Kd = 0.34 nM, Bmax = 2.2 nmol/g protein and Hill No. = 1.01. Triton X-100 at 5 x 10(-4)% inhibited the specific binding of [3H]QNB and the inhibition was almost complete at 10(-2)%. Treatment with 2.5 x 10(-6) M atropine, followed by centrifugation washings protected the receptor site from the inhibitory action of the detergent. The protection afforded by other cholinergic drugs was less effective. The use of this technique has confirmed the results of our previous work on the possible pre- and postsynaptic location of central muscarinic receptors. These findings open the possibility for protection of other detergent-sensitive receptors and for their isolation and purification as well-defined macromolecules.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Aguilar JS,Criado M,De Robertis Edoi
10.1016/0014-2999(80)90252-6subject
Has Abstractpub_date
1980-05-16 00:00:00pages
251-7issue
4eissn
0014-2999issn
1879-0712pii
0014-2999(80)90252-6journal_volume
63pub_type
杂志文章abstract::Given the differences in the dopamine neurotransmission between the shell and the core of the nucleus accumbens, as well as the differential involvement of these two domains in oral behaviour of rats, it was decided to determine whether or not dopamine D1 and/or dopamine D2 receptors differentially direct oral behavio...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00428-n
更新日期:1995-11-03 00:00:00
abstract::Long-term treatment with sodium barbital did not alter significantly the responsiveness of the isolated rat vas deferens to noradrenaline. However, three days after barbital withdrawal there was a 4.5-fold increase in the sensitivity and an enhanced maximum response to the neurotransmitter. Pharmacological analysis of...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90550-7
更新日期:1982-08-13 00:00:00
abstract::Amitriptyline is known to increase the permeability of the blood-brain barrier but the morphological basis of this increase has not been studied. As catecholamines can influence pinocytosis in dog peripheral blood vessels, the effect of amitriptyline on the pinocytotic activity of blood brain microvessels was studied....
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90133-q
更新日期:1990-01-25 00:00:00
abstract::Cocaine is eliminated and detoxified principally through the metabolism of nonspecific plasma and tissue esterases. Microsomal oxidative metabolism is of importance in cocaine N-demethylation, this being a principal pathway of cocaine bioactivation and hepatotoxicity. The contribution of different cytochrome P450 (CYP...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0926-6917(94)90078-7
更新日期:1994-01-03 00:00:00
abstract::This paper presents the effect of 14-day intraperitoneal (i.p.) neuroleptic treatment on the behavioural response of Wistar rats to (-)-quinpirole hydrochloride (3 mg/kg, i.p.) administered 24 h after the last neuroleptic dose. Chlorpromazine hydrochloride (10 mg/kg), haloperidol (2 mg/kg) or (+/-)-sulpiride (100 mg/k...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(99)00666-4
更新日期:1999-11-19 00:00:00
abstract::Guanosine 3',5'-cyclic monophosphate (cGMP) is an important second messenger in many biological systems including vascular smooth muscle where it mediates relaxation. Cellular levels of cGMP are regulated primarily by three enzymes; nitric oxide (NO) synthase, soluble guanylate cyclase, and cGMP-phosphodiesterase. Bas...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00307-0
更新日期:1998-06-19 00:00:00
abstract::C-type natriuretic peptide (CNP) is the major natriuretic peptide in the brain and its mRNA has been reported in the central nervous system, which supports local synthesis and its role as a neuromodulator. The aim of the present work was to study the effect of centrally applied CNP on pancreatic secretion. Rats were f...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2005.09.015
更新日期:2005-11-07 00:00:00
abstract::We examined whether the proteinase-activated receptor-2 (PAR2) agonist, H-Ser-Leu-Ile-Gly-Arg-Leu-NH2 (SLIGRL-NH2), could induce scratching behavior in mice. Intradermal injections of SLIGRL-NH2 (10-50 microg) evoked dose dependent scratching. This behavior peaked near 5 min and returned to preinjection levels within ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2005.11.012
更新日期:2006-01-20 00:00:00
abstract::Statin medications diminish cholesterol biosynthesis and are commonly prescribed to reduce cardiovascular disease. Statins also reduce production of ubiquinol, a vital component of mitochondrial energy production; ubiquinol reduction may contribute to rhabdomyolysis. Human rhabdomyosarcoma cells were treated with eith...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.04.009
更新日期:2013-07-05 00:00:00
abstract::The endocannabinoids anandamide (AEA) and 2-arachidonoylglycerol (2-AG) are metabolised by cells by hydrolysis to arachidonic acid followed by esterification into phospholipids. Here, we report that nitric oxide (NO) donors significantly increase the amount of tritium accumulated in the cell membranes of RBL2H3 rat ba...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2009.08.028
更新日期:2009-10-25 00:00:00
abstract::The effects of H 25 and H 74 on ouabain-resistant 86Rb+ influx were tested in beta-cell-rich mouse pancreatic islets. Both H 25, which is considered to be a specific inhibitor of Na+, K+, Cl- co-transport, and H 74, a specific inhibitor of K+, Cl- co-transport, reduced the ouabain-resistant 86Rb+ influx. The specific ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90875-i
更新日期:1993-07-20 00:00:00
abstract::To determine the role of protein kinase C in the regulation of intestinal fluid transport, experiments were performed with the rat jejunum in vivo, using the active phorbol ester, 4-beta-phorbol 12-myristate 13-acetate (PMA), as stimulator of protein kinase C. Intraluminally administered PMA dose dependently reversed ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90053-9
更新日期:1990-07-17 00:00:00
abstract::The administration of the synthetic and stable opioid peptide[D-Ala2,MePhe4,Met(O)5o1]enkephalin (FK 33-824) at the dose of 0.2 mg/kg i.v. induced a rise in plasma levels of prolactin in the rat, an effect which was prevented by 1 mg/kg i.v. of the opiate antagonist naloxone. A simultaneous i.v. injection of 20 microg...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90009-7
更新日期:1982-01-22 00:00:00
abstract::The effect of colchicine on jejunal adenylate cyclase activity, prostaglandin E2 (PGE2) and cAMP contents, the enzyme and mediators involved in intestinal fluid secretion was tested in rats. Four h after the intraperitoneal injection of colchicine (0.5 mg/100 g body wt.) mucosal PGE2 content, adenylate cyclase activit...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(80)90503-8
更新日期:1980-10-17 00:00:00
abstract::The cardiovascular effects of atriopeptins (AP) I, II and III were compared in spontaneously beating or electrically stimulated guinea pig atria and in rabbit aortic strips precontracted by various agonists. Atriopeptins did not significantly affect sinus nodal rate or atrial contractility. AP II and III, although mor...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90224-9
更新日期:1985-04-02 00:00:00
abstract::Osthole is a coumarin extracted from Cnidium monnieri (L.) Cusson. The medicinal plant is widely used in Vietnamese as well as Chinese traditional medicine as a vasodilating and antihypertensive agent. Here we have tested the proposition that the block of Ca(v)1.2 channels is mainly responsible for its vascular activi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.01.038
更新日期:2012-04-05 00:00:00
abstract::Pretreatment with the non-competitive NMDA (N-methyl-D-aspartate) antagonist MK801 (0.5, 1.0 mg/kg, s.c.) suppressed the behavioral signs of withdrawal in morphine-dependent rats. However, the same doses of MK801 that suppressed morphine withdrawal also simultaneously produced phencyclidine (PCP)-like behaviors. Pretr...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90358-w
更新日期:1991-05-02 00:00:00
abstract::In primary cultured striatal neurons we found that (+-)-trans-1-amino-cyclopentyl-1,3-dicarboxylate (trans-ACPD) could inhibit forskolin-induced cAMP formation in a dose-dependent manner (EC50 156 +/- 38 microM, n = 5, maximal inhibition 37.8 +/- 1.2, n = 37). The trans-ACPD-induced inhibition was totally abolished in...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(92)90112-9
更新日期:1992-04-10 00:00:00
abstract::We previously reported that the functional deletion of p21, a cyclin-dependent kinase inhibitor, in mice attenuated renal cell senescence in streptozotocin (STZ)-induced type 1 diabetic mice. In the present study, we investigated the effect of iron chelation on renal cell senescence and inflammation in the type 1 diab...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2015.03.053
更新日期:2015-06-05 00:00:00
abstract::Toll-like receptors (TLRs) play an important role in the recognition of microbial pathogens and induce innate immune responses. The recognition of microbial components by TLRs triggers the activation of myeloid differential factor 88 (MyD88)- and toll-interleukin-1 receptor domain-containing adapter inducing interfero...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.09.045
更新日期:2013-12-05 00:00:00
abstract::Thaliporphine (0.1-100 microM) produced sustained, concentration-dependent contraction in isolated rings of rat aorta. Thaliporphine (ED50 = 1.5 +/- 0.5 microM) was less potent than endothelin (ED50 = 3.9 +/- 0.4 nM), but was more potent than Bay K 8644 (ED50 = 5.5 +/- 0.6 microM). Thaliporphine also contracted guinea...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90342-f
更新日期:1993-03-16 00:00:00
abstract::Growing evidence supports involvement of low-affinity/high-capacity organic cation transporters (OCTs) and plasma membrane monoamine transporter (PMAT) in regulating clearance of monoamines. Currently decynium-22 (D22) is the best pharmacological tool to study these transporters, however it does not readily discrimina...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2018.10.028
更新日期:2019-01-05 00:00:00
abstract::Oxidative stress is proved to be harmful to the vascular endothelial cells which are important in preventing the formation and progression of atheromatous plaque. This study was designed to investigate the protective effect and potential mechanisms of dihydrotestosterone (DHT) against H(2)O(2)-induced apoptosis of hum...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2010.06.039
更新日期:2010-09-25 00:00:00
abstract::Dynorphin (1-100 nM) dose dependently inhibited both spontaneous and electrically evoked endogenous dopamine (DA) release from slices of the nucleus accumbens of untreated rats. When this inhibitory effect was compared, it was significantly reduced in rats pretreated (for 9 days) with methamphetamine (6 mg/kg per day ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)90461-c
更新日期:1992-11-03 00:00:00
abstract::Human adipose tissue-derived stromal cells (hADSCs) demonstrate promising potential in various clinical applications, including the transplantation to regenerate injured or degenerative tissues. The migration of engrafted hADSCs to the correct site of injure is essential for the curative effect of stem cell therapy. W...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.09.030
更新日期:2008-12-03 00:00:00
abstract::We determined the role of high-grade inflammation on endothelial function and its association with biomarkers of endothelial dysfunction in collagen-induced arthritis. Sprague-Dawley rats were divided into a control (n = 12) or collagen-induced arthritis (CIA; n = 21) group. To induce arthritis, Bovine-type-II collage...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2019.172786
更新日期:2019-12-15 00:00:00
abstract::The manner in which arachidonic acid and other free fatty acids influence the vesicular uptake of glutamate and gamma-aminobutyric acid (GABA) has been investigated. The cis-polyunsaturated fatty acid arachidonic acid (20:4), eicosapentanoic acid (20:5) and linolenic acid (18:3) at 150 nmol/mg protein (50 microM) inhi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01449-0
更新日期:1998-01-12 00:00:00
abstract::In rat carotid arteries isolated 2 weeks after balloon denudation, a significant neointima developed with little change in medial size. Associated with this neointimal hyperplasia was a marked decrease in contraction to various agents including angiotensins I and II, big endothelin-1, endothelin-1, norepinephrine, phe...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90610-6
更新日期:1994-04-11 00:00:00
abstract::Several aspects of the role of corticotropin-releasing factor (CRF) in the forced swimming test were investigated in this study by using two different administration schedules. I.c.v. microinjection of CRF produced a dose-dependent increase in swimming activity when the administration schedule originally reported for ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01515-x
更新日期:1998-02-05 00:00:00
abstract::In the presence of thiorphan an 'enkephalinase' inhibitor, bestatin an aminopeptidase inhibitor of bacterial origin potently inhibited the hydrolysis of [3H][Leu5]enkephalin by slices from rat striatum with an IC50 value of about 0.2 microM whereas puromycin was approximately 1000 times less potent on this preparation...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(83)90181-4
更新日期:1983-01-21 00:00:00