Abstract：
:Carbachol produces both negative and positive inotropy in rat left atria. It is not clear whether these two effects are mediated by two separate cell surface muscarinic receptors or a single receptor interacting with two coupling proteins in the cell membrane. Pirenzepine, known to selectively block some biochemical muscarinic responses, was used in this study to block the biphasic response to carbachol in rat left atria. The negative inotropy to carbachol was blocked by pirenzepine, and Schild analysis indicated a -log dissociation constant (pKb) for the pirenzepine-receptor complex of 6.2. However, the Schild analysis may have been complicated by positive inotropy observed with pirenzepine. This positive inotropic effect was sensitive to blockade by other muscarinic antagonists. In atria from rats pretreated with pertussis toxin, carbachol produced a positive inotropic effect. Schild analysis with pirenzepine for antagonism of this response indicated a -log equilibrium dissociation constant for the pirenzepine-receptor complex of 6.7, significantly different from that for antagonism of negative inotropy. This ostensibly suggested a difference in the receptors mediating these responses. In view of the possible complicating effects of the positive inotropic effects of pirenzepine in this assay, an alternative method for the measurement of pirenzepine affinity was utilized. Resultant analysis was used to measure the pKb for pirenzepine antagonism of negative inotropy to carbachol. This method had the advantage of cancelling the positive inotropy to pirenzepine. Under these circumstances, pirenzepine had a pKb of 6.9, a value not significantly different from for antagonism of the positive inotropy to carbachol. The relevance of these findings is discussed in terms of a single promiscuous muscarinic receptor or heterogeneous receptors in this tissue. These data do not support the hypothesis that two separate receptors mediate these two effects.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Boselli C,Kenakin TPdoi
10.1016/0014-2999(90)94095-fsubject
Has Abstractpub_date
1990-11-20 00:00:00pages
49-57issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(90)94095-Fjournal_volume
191pub_type
杂志文章abstract：:The impacts of prenatal propofol on cognition and emotion of offspring remain elusive. In the present study, pregnant rats in the second trimester were anesthetized with propofol. Neuronal apoptosis and proliferation was determined in fetuses and postnatal rats by detecting caspase-3 and BrdU expression. The offspring...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.11.032
更新日期：2019-01-15 00:00:00
abstract：:Induction of anaphylactic shock in mice by i.v. antigen challenge (bovine serum albumin, 100 micrograms) or i.v. treatment with the mast cell degranulator compound 48/80 resulted in 80 and 90% mortality rate, respectively. Inhibition of nitric oxide (NO) synthesis from L-arginine by co-injection of the L-arginine anal...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90800-6
更新日期：1991-10-02 00:00:00
abstract：:We have monitored the binding of [125I]thienylphencyclidine ([125I]TCP), a novel high affinity radioiodinated ligand that specifically recognizes the NMDA (N-methyl-D-aspartate) receptor in rat brain membranes. [125I]TCP binds with an affinity of about 30 nM, and recognizes a similar number of binding sites to previou...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(92)90082-7
更新日期：1992-05-12 00:00:00
abstract：:This study investigates the anti-inflammatory effects of 1-(2-chlorophenyl)-N-methyl-N(1-methylpropyl)-3-isoquinoline carboxamide and 7-chloro-5-(4-chlorophenyl)-1, 3-dihydro-1-methyl-2-H-1,4-benzodiazepin-2-one in paw oedema induced by carrageenan in mice. Pretreatment (24 h) with both ligands inhibited oedema format...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00745-1
更新日期：1999-12-03 00:00:00
abstract：:Rats were treated with ethanol in the drinking fluid 2 X 1 h daily for 83 weeks. [3H]Muscimol, [3H]quinuclidinyl benzilate ( [3H]QNB) and [3H]nicotine binding was measured in selected brain areas 7, 14 and 21 days after withdrawal of ethanol. A significant increase (P less than 0.05) when compared to controls was foun...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90704-6
更新日期：1985-09-24 00:00:00
abstract：:Depression and cocaine use disorder represent frequent co-current diagnoses and the GABAB receptors are involved in both conditions. This research involved the application of the animal model of depression (bulbectomy, OBX) and cocaine use disorder (self-administration) to assess the efficiency of GABAB receptor agoni...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173324
更新日期：2020-09-15 00:00:00
abstract：:Pharmacological strategies aimed at co-activating peroxisome proliferator-activated receptor-gamma (PPAR-γ)/nuclear factor erythroid 2-related factor 2 (Nrf2) pathway have shown promising results in alleviating myocardial injury. The aim of the study was to evaluate the role of chrysin, a PPAR-γ agonist, in ischemia-r...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173389
更新日期：2020-09-15 00:00:00
abstract：:The hypotensive activity of a series of calcium entry blockers and various other vasodilators was quantified in pentobarbitone-anesthetized rats. Hypotensive activity was correlated linearly with the potency of these vasoactive agents to depress alpha 2-adrenoceptor-induced pressor responses in pithed rats. However, v...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90104-8
更新日期：1983-08-19 00:00:00
abstract：:Curcumin, main compound obtained from rizhoma of Curcuma longa, shows antitumoral, antioxidant, anticarcinogenic and gastric protective properties. Recently, it has been demonstrated that curcumin exerts its gastric protective action due to an increase in gastric nitric oxide (NO) levels. However, it is unknown whethe...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.02.030
更新日期：2014-05-05 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：:Hypoglycemia developed in fasted rats during forced swimming. This hypoglycemia was mostly abolished by phentolamine, an alpha-adrenolytic agent, or by hexamethonium; was potentiated by propranolol, a beta-adrenolytic agent, of by 5-methoxyindole-2-carboxylic acid, a gluconeogenic inhibitor; and was not affected by an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90184-4
更新日期：1977-03-07 00:00:00
abstract：:The involvement of brain monoamines in the mechanism of action of nefopam, a new analgesic, was investigated in rats. The study was designed to evaluate the effect of various means of impairing monoaminergic transmission on nefopam analgesia as measured with the hot plate method. Pretreatment with reserpine (2 mg/kg) ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90762-4
更新日期：1986-09-09 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：:Forskolin, a potent activator of adenylate cyclase, and isoprenaline, an unselective beta-adrenoceptor agonist, were studied in vitro on tissues from guinea-pig with respect to relaxation of the carbachol-contracted trachea, increase in the force of contraction of the papillary muscle and depression of subtetanic cont...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90780-0
更新日期：1985-06-19 00:00:00
abstract：:The endocannabinoid system appears to have an important role in specific aspects of learning and memory, yet there has been no systematic study of the role of cannabinoid receptors in contextual fear conditioning. The present study examined the effects of cannabinoid CB(1) receptor blockade on the acquisition, consoli...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.04.017
更新日期：2006-06-13 00:00:00
abstract：:Acute administration of delta 9-tetrahydrocannabinol (THC) (50 mg/kg) at puberty (35-40 days) significantly (P less than 0.05) reduced Ca2+ ATPase activity in hypothalamic plasma membranes but increased, although not significantly, enzyme activity in hypothalamic tissue obtained from adult mice. In contrast, testicula...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90186-5
更新日期：1987-05-07 00:00:00
abstract：:The antihypertensive drug doxazosin has been associated with an increased risk for congestive heart failure and cardiomyocyte apoptosis. Human ether-a-go-go-related gene (hERG) K(+) channels, previously shown to be blocked by doxazosin at therapeutically relevant concentrations, represent plasma membrane receptors for...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.10.051
更新日期：2008-01-28 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
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90219-9
更新日期：1982-12-03 00:00:00
abstract：:Store-operated Ca2+ entry is referred to a capacitative current activated by Ca2+ -stores depletion in various non-excitable cells. Neutrophil-like HL-60 cells responded to N-formyl-L-Methionyl-L-Leucyl-L-Phenylalanine (fMLP) by an early O2- production preceded by a [Ca2+]i rise. Cell stimulation in the absence of ext...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00728-6
更新日期：1998-11-20 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01203-x
更新日期：1997-09-24 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.09.060
更新日期：2011-01-10 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90456-z
更新日期：1991-06-25 00:00:00
abstract：:Two inhibitors of the cellular uptake of the endocannabinoid anandamide, (R)-N-oleoyl-(1'-hydroxybenzyl)-2'-ethanolamine and (S)-N-oleoyl-(1'-hydroxybenzyl)-2'-ethanolamine (OMDM-1 and OMDM-2, respectively), were recently synthesized, and their in vitro pharmacological activity described. Here we have assessed their a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2003.11.027
更新日期：2004-01-26 00:00:00
abstract：:The effect of intrathecal clonidine on thermal nociception and hindlimb flexion was assessed in acute and chronic spinally transected rats. After an acute, 1-day spinalization, there was no change in the antinociceptive dose-response function to clonidine, relative to intact rats. However, there was a significant incr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01259-1
更新日期：2002-02-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.11.019
更新日期：2008-02-12 00:00:00
abstract：:Methylxanthines increase central noradrenergic turnover by an unknown mechanism. Isobutyl methylxanthine (IBMX, 0.5-16 mg/kg i.v.) was found in this study to increase firing rats of noradrenergic neurons in the locus coeruleus, supporting increased impulse flow as one possible mechanism for increased noradrenergic tur...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90430-7
更新日期：1982-11-05 00:00:00
abstract：:The pharmacological characteristics of the binding of [3H]8-OH-DPAT ([3H]8-hydroxy-2(di-n-propylamino)tetralin, [125I]CYP ((-)[125I]iodocyanopindolol) (in the presence of 30 microM (-)isoprenaline) and [3H]mesulergine to 5-HT1 recognition sites were studied in rat and pig brain membranes. [3H]8-OH-DPAT bound in rat an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90658-2
更新日期：1985-11-26 00:00:00
abstract：:Nicotine acts as an agonist of nicotinic acetylcholine receptors. Nicotinic acetylcholine receptors play a role in the modulation of neurotransmitter release in both the central and the peripheral nervous system. Moderate reactive oxygen species levels modulate the regulation of physiological functions e.g. neurotrans...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.03.029
更新日期：2008-06-10 00:00:00
abstract：:Jolkinolide B (JB), which is isolated from the dried root of Euphorbia fischeriana Steud., has been reported to possess various therapeutic effects, such as treatment of edema and abdominal distention and protection against acute lung injury, and it has also been reported to have anti-inflammatory even antitumor prope...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.10.025
更新日期：2019-01-05 00:00:00
abstract：:In this study we demonstrate allograft survival in a rat model of renal transplantation using the delta1-opioid receptor antagonist, 7-(benzospiroindanyl)naltrexone [corrected]. Treatment with 7-(benzospiroindanyl)naltrexone [corrected] caused 50% of the rats to survive longer than 100 days (untreated, 11 +/- 3 days)....
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00477-4
更新日期：1998-07-31 00:00:00
