Abstract：
:Procaine and procainamide were covalently bound to acryloyl monomers and polymers. The dose-response and time-action parameters of the cardiac antiarrhythmic protection afforded by the prototype drugs and their acryloyl derivatives against chloroform-hypoxia-induced cardiac arrhythmias in unanesthetized mice and epinephrine-induced arrhythmias in alpha-chloralose anesthetized cats were determined. Similarly, the pharmacological parameters which characterized their acute toxic responses in unanesthetized male albino mice were also determined. The similar pharmacological spectra of their activity and the parallelism of their lethal dose-response curves indicate that the active constituents of the polymer derivatives are the local anesthetic moieties. Compared to the prototype drugs, the polymer derivatives were more potent on a molar basis and their pharmacological effects were prolonged. The increased potency and duration of action reinforce the idea that the local anesthetic moieties are pharmacologically active while still bound to the polymer backbones.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Erker EF,Baker T,Okamoto M,Udenfriend S,Riker WF Jrdoi
10.1016/0014-2999(85)90367-xsubject
Has Abstractpub_date
1985-08-27 00:00:00pages
253-9issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(85)90367-Xjournal_volume
114pub_type
杂志文章abstract：:We investigated the effects of L-arginine and NG-nitro-L-arginine methyl ester (L-NAME) on macromolecule extravasation in the microcirculation of awake hamsters by computer-assisted image analysis of the distribution of FITC (fluorescein isothiocyanate)-dextran fluorescence in dorsal fold skin preparations. This analy...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00045-4
更新日期：1998-04-10 00:00:00
abstract：:Increasing concentrations of the functional antagonist carbachol resulted in a shift to the right of the dose-response curves for (--)-isoproterenol-induced positive chronotropic and inotropic responses and a reduction of the maximum degree of response that could be produced relative to that produced by theophylline. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90233-9
更新日期：1978-02-01 00:00:00
abstract：:The acute effects of propranolol, 1 mg/kg i.v., were studied in chloralosed, vagotomized cats. The vascularly isolated but innervated calf muscles were perfused from another animal. In one group of experiments, the carotid baroreceptors were exposed to ambient arterial pressure. Here, propranolol caused a fall in hear...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90361-8
更新日期：1978-08-01 00:00:00
abstract：:The effect of dextromethorphan on several types of cation currents in cultured rat cortical neurons and PC12 cells was studied by using the whole-cell configuration of the patch-clamp technique. The Ba2+ current through L- and N-type Ca2+ channels was blocked with similar potencies (52-71 microM) in both types of cell...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90849-d
更新日期：1993-07-20 00:00:00
abstract：:The gastric anti-secretagogue effects of cimetidine (a histamine H2-receptor antagonist) and of atropine (a non-selective muscarinic receptor antagonist) and pirenzepine (a selective muscarinic M1-receptor antagonist) were examined in conscious gastric fistula rats both under basal conditions and after stimulation wit...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90436-5
更新日期：1987-06-19 00:00:00
abstract：:The main goal of this project was to study the effect of amiodarone upon ventricular fibrillation and defibrillation thresholds (VFT and VDT) in the canine heart under normal and ischemic conditions. Both parameters were assessed in 11 dogs, each experiment consisting of three consecutive phases: (a) control, which re...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90079-8
更新日期：1986-06-05 00:00:00
abstract：:The tertiary nitrogen derivatives of two choline esters, chloroacetylcholine and acrylcholine, known to inhibit choline acetyltransferase (ChAc) in vitro, were tested for their effects in the whole animal, including peripheral and central cholinergic systems. These esters are N,N-dimethylaminoethyl chloroacetate (Cl-D...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90357-5
更新日期：1976-11-01 00:00:00
abstract：:The aim of the present study was to determine the effect of a calcium channel blocker on renal function, urinary endothelin excretion and endothelin receptor number in rats. Administration of cyclosporine resulted in a significant impairment of renal function when measured by either [14C]inulin or 24 h creatinine clea...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90132-a
更新日期：1991-02-26 00:00:00
abstract：:A microdialysis/smallbore chromatographic system was used to monitor changes in extracellular dopamine concentration in the striatum of the rat following administration of drugs that block catecholamine uptake. Analysis of 0.5 microliter of dialysate every 5 min showed dose-dependent elevations in extracellular dopami...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90592-9
更新日期：1987-07-23 00:00:00
abstract：:Oxidative stress has been implicated in the pathogenesis of acute myocarditis. The imbalance between the occurrence of reactive oxygen species and the cellular antioxidant defense mechanism plays a key role in myocardial injury of viral myocarditis. Carvedilol, a nonselective beta-adrenoceptor antagonist with addition...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.04.037
更新日期：2010-08-25 00:00:00
abstract：:Spinal 5-HT1A receptor subtypes are involved in regulation of nociception. This study was performed to investigate the effect of stimulation of these receptors on wide dynamic range neurones in the spinal cord. Extracellular single unit recordings of dorsal horn neurones were performed in intact urethane-anaesthetized...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00819-9
更新日期：1996-12-30 00:00:00
abstract：:We investigated the acute and chronic effects of alpha 2-adrenoceptor and muscarinic receptor agonists on dihydropyridine-sensitive voltage-dependent Ca2+ channels in spinal cord-dorsal root ganglion cocultures. Clonidine and oxotremorine inhibited the voltage-dependent Ca2+ influx (42 +/- 2% and 35 +/- 6% with 100 mi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(93)90060-m
更新日期：1993-01-04 00:00:00
abstract：:Angiotensin II increased the inositol phosphates production (EC50 = 3.4+/-0.7 nM) in Chinese hamster ovary (CHO) cells expressing the cloned human angiotensin AT1 receptor (CHO-AT1 cells). Coincubation with angiotensin AT1 receptor antagonists produced parallel rightward shifts of the concentration-response curve with...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00205-8
更新日期：1999-05-14 00:00:00
abstract：:We review a large volume of literature concerning mathematical models of cancer therapy, oriented towards optimization of treatment protocols. The review, although partly idiosyncratic, covers such major areas of therapy optimization as phase-specific chemotherapy, antiangiogenic therapy and therapy under drug resista...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2009.08.041
更新日期：2009-12-25 00:00:00
abstract：:The effects of caffeine (10 mM) on depolarization-activated, calcium-independent outward K+ currents were investigated in isolated rat ventricular myocytes, using whole-cell clamping. The external solution contained CoCl2 2 mM and the internal solution contained ethylene glycol-bis(-aminoethyl ether) N,N,N',N'-tetraac...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90551-e
更新日期：1992-12-15 00:00:00
abstract：:To determine if an Ag(+)-induced contracture is associated with the Ca(2+)-induced Ca2+ release mechanism in the sarcoplasmic reticulum, effects of Ca(2+)-induced Ca2+ release modulators on the Ag(+)-induced contracture were studied with single fibers of frog toe skeletal muscle. The fiber treated with 1 mM caffeine c...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0926-6917(95)90036-5
更新日期：1995-03-16 00:00:00
abstract：:The present study was conducted with an aim to explore the possible role of naringin against ischemia reperfusion induced-neurobehavioral alterations, oxidative damage, cellular and histopathological alterations in cortex, striatum, hippocampus areas of brain. Male Wistar rats (200-220 g) were subjected to bilateral c...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.06.056
更新日期：2009-08-15 00:00:00
abstract：:Osteoarthritis (OA) is a common yet destructive disease affecting the articular cartilage, and is a major cause of immense suffering and disability for millions of people. Previous studies have shown that triptolide (TPL), an active compound derived from Tripterygium wilfordii, has potent immunosuppressive and anti-in...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173341
更新日期：2020-09-15 00:00:00
abstract：:The functional role of P2X7 receptor (P2X7R) inhibition in cancer-induced bone pain has been highly contradictory. Whereas knockout studies have suggested pro-nociceptive effects, pharmacological studies suggest anti-nociceptive or no effect. The discrepancy is likely linked to the highly polymorphic nature of the P2X...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.12.032
更新日期：2019-02-15 00:00:00
abstract：:EMD 57445 ((S)-(-)-[4-hydroxy-4-(3,4-benzodioxol-5-yl) -piperidin-1-ylmethyl]-3-(4-methoxyphenyl)-oxazolidin- 2-one) is a new sigma receptor ligand with only marginal affinity for many other (including dopamine) receptors. In the present study, central, particularly neuroleptic-like, effects of this compound were eval...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00602-4
更新日期：1996-11-21 00:00:00
abstract：:There is some controversy as to whether 5-HT(2C) receptor agonists are anxiogenic or anxiolytic. The effects of the novel 5-HT(2C) receptor agonist, (S)-2-chloro-5-fluoro-indol-1-yl)-1-methyl ethylamine fumarate (RO 60 0175), in three models of anxiety were therefore tested. RO 60 0175 was found to induce hypolocomoti...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00706-2
更新日期：2000-01-10 00:00:00
abstract：:The ability of the prostacyclin (IP) receptor agonist cicaprost to activate Gs-, Gq/11- and Gi-mediated cell signalling pathways has been examined in Chinese hamster ovary (CHO) cells and human embryonic kidney 293 (HEK 293) cells expressing the cloned human (hIP) or mouse (mIP) prostacyclin receptor, and compared wit...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)02006-5
更新日期：2003-08-01 00:00:00
abstract：:The present study describes the effects of halothane on morphine activity in the isolated left atria of the rat. Concentration-response curves were obtained for the negative inotropic effects of morphine on electrically stimulated left atria. Morphine significantly decreased the contractile force, with an inhibitory c...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90566-o
更新日期：1990-01-17 00:00:00
abstract：:The involvement of tachykinin NK1 receptors in the plasma protein extravasation (measured by the Evans blue leakage technique) produced by intravenous administration of capsaicin was investigated in the urinary bladder and trachea of anesthetized rats. Capsaicin-induced plasma extravasation was markedly inhibited by (...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90183-q
更新日期：1991-12-17 00:00:00
abstract：:When injected directly into the tail, U50,488H is a potent analgesic in the tailflick assay (ED50 3.1 micrograms). The analgesic activity is lost if the radiant heat is focused 1 cm away from the site of injection. The kappa 1-opioid receptor antagonist nor-binaltorphimine given systemically reverses the local analges...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00520-1
更新日期：1996-08-29 00:00:00
abstract：:Opiate agonists exhibiting selectivity for mu, kappa, sigma, and delta opiate receptors were microinjected into the periaqueductal gray region (PAG) of the brain of rats to determine the receptor subtype(s) associated with the initiation of descending pain inhibition. The spinally organized, heat nociceptive tail-flic...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90145-8
更新日期：1988-10-26 00:00:00
abstract：:The effect of peripheral and intrathecal administration of the bradykinin B2 receptor antagonist HOE140 and the non-steroidal anti-inflammatory drug indomethacin were studied on the response of dorsal horn nociceptive neurones to formalin in the anaesthetized rat. Peripheral pretreatment with HOE140 reduced both phase...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90484-l
更新日期：1992-09-04 00:00:00
abstract：:The actions of iontophoretically applied quipazine (QPZ) and 6-chloro-2-[1-piperazinyl]-pyrazine (CPP) were compared with those of serotonin (5-HT) on rat spinal motoneurones. QPZ and CPP qualitatively resembled 5-HT in that both facilitated single unit activity evoked by glutamate. Like 5-HT, the facilitation they pr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90600-8
更新日期：1982-06-16 00:00:00
abstract：:We have investigated the role of tyrosine kinase in the antiarrhythmic effects of peroxynitrite preconditioning in rat isolated heart by using a tyrosine phosphatase inhibitor, sodium orthovanadate, and tyrosine kinase inhibitors, genistein and tyrphostin. Rat hearts were preconditioned by peroxynitrite administration...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01377-3
更新日期：2003-03-19 00:00:00
abstract：:The protective potency of ischemic preconditioning decreases with increasing age. A key step in ischemic preconditioning is the opening of mitochondrial Ca(2+) sensitive K(+) (mK(Ca)) channels, which causes mild uncoupling of mitochondrial respiration. We hypothesized that aging reduces the effects of mK(Ca) channel o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.09.008
更新日期：2008-01-14 00:00:00
