Phenoxybenzamine is more potent in inactivating alpha 1- than alpha 2-adrenergic receptor binding sites.

Abstract:

:The effects of phenoxybenzamine on alpha 1- and alpha 2-adrenergic receptor binding sites were examined directly using radioligand binding assays of the antagonist drugs [125I]BE 2254 and [3H]rauwolscine, respectively, in homogenates of rat cerebral cortex. Treatment with phenoxybenzamine caused an irreversible, dose-dependent decrease in the density of both alpha 1- and alpha 2-adrenergic receptors. Phenoxybenzamine was approximately 250-fold more potent at decreasing alpha 1-adrenergic receptor density than it was at decreasing alpha 2-adrenergic receptor density.

journal_name

Eur J Pharmacol

authors

Minneman KP

doi

10.1016/0014-2999(83)90458-2

subject

Has Abstract

pub_date

1983-10-14 00:00:00

pages

171-4

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(83)90458-2

journal_volume

94

pub_type

杂志文章
  • The effect of Eleutheroside E on behavioral alterations in murine sleep deprivation stress model.

    abstract::Eleutheroside E (EE), a principal component of Eleutherococcus senticosus, has been reported to have anti-inflammatory and protective effects in ischemia heart etc. However, whether it can mitigate behavioral alterations induced by sleep deprivation, has not yet been elucidated. Numerous studies have demonstrated that...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.02.036

    authors: Huang LZ,Wei L,Zhao HF,Huang BK,Rahman K,Qin LP

    更新日期:2011-05-11 00:00:00

  • Effects of oxidized low-density lipoprotein on differentiation of mouse neural progenitor cells into neural cells.

    abstract::In Alzheimer's disease (AD), a decline in function of neural progenitor cells (NPCs) results in a reduced capacity for neural regeneration. It has been shown that plasma oxidized low-density lipoprotein (ox-LDL) levels are positively correlated with severity in patients with AD. However, the direct effects of ox-LDL o...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173456

    authors: Ishizuka T,Nagata W,Nomura-Takahashi S,Satoh Y

    更新日期:2020-12-05 00:00:00

  • Phosphodiesterase 4-dependent regulation of cyclic AMP levels and leukotriene B4 biosynthesis in human polymorphonuclear leukocytes.

    abstract::Several selective phosphodiesterase 4 inhibitors were found to be potent inhibitors of the N-formyl-Met-Leu-Phe (fMLP)-induced leukotriene B4 biosynthesis by human polymorphonuclear leukocytes with IC50s in the nanomolar range (0.09-26 nM). The rank order of potency was 6-(4-pyridylmethyl)-8-(3-nitrophenyl)quinoline (...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00987-x

    authors: Denis D,Riendeau D

    更新日期:1999-02-19 00:00:00

  • Epithelial modulation of the relaxant activity of atriopeptides in rat and guinea-pig tracheal smooth muscle.

    abstract::Three peptide components of atrial natriuretic factor (ANF) caused relaxation of carbachol-contracted guinea-pig isolated tracheal smooth muscle. These were the 1-28, 5-28 and 5-27 peptide sequences (ANF(1-28), ANF-(5-28) and ANF-(5-27)). The peptides were 10-30 times more potent in epithelium-denuded than in epitheli...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90328-2

    authors: Fernandes LB,Preuss JM,Goldie RG

    更新日期:1992-03-03 00:00:00

  • Short-term prophylaxis with deoxyspergualin prevents testicular autoimmunity in mice.

    abstract::The effects of the treatment with the immunosuppressant deoxyspergualin on the development of experimental autoimmune orchitis were studied. The results showed that C3H/He mice immunized with testicular germ cells and treated daily with either 0.3 or 3 mg/kg body weight deoxyspergualin during days 15-20 post-immunizat...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)02045-9

    authors: Ablake M,Itoh M,Kaneko T,Iimura A,Nakamura Y,Meroni P,Nicoletti F

    更新日期:2002-08-23 00:00:00

  • Comparison of two alpha-noradrenergic agonists (clonidine and guanfacine) on norepinephrine turnover in the cortex of rats during morphine abstinence.

    abstract::The effects of the alpha-agonists clonidine and guanfacine on rat cortical norepinephrine turnover during morphine withdrawal were assessed. Cortical norepinephrine levels were measured, after administration of alpha-methyl-p-tyrosine, by fluorometric assay. Chronic treatment with morphine did not affect norepinephrin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(81)90368-x

    authors: Zigun JR,Bannon MJ,Roth RH

    更新日期:1981-04-09 00:00:00

  • 3H-noradrenaline outflow induced from isolated aventitia and intima-media of rabbit aorta by electrical field stimulation.

    abstract::Electrical field stimulation of the isolated adventitial and intima-medial layers of rabbit aorta preloaded with 3H-noradrenaline elicited a 3H outflow. The initial 3H outflow from adventitia was independent of external Ca2+ concentration. Each of the subsequent 3H outflows was mainly Ca2+ sensitive. All stimulation-i...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(76)90156-4

    authors: Schrold J,Nedergaard OA

    更新日期:1976-10-01 00:00:00

  • Nitric oxide induces apoptosis associated with TRPV1 channel-mediated Ca(2+) entry via S-nitrosylation in osteoblasts.

    abstract::The high-level production of nitric oxide (NO) induced by inflammatory cytokines has been shown to play a key role in the pathogenesis of inflammation-mediated osteoporosis. In the present work, we observed that 1mM of the NO donor sodium nitroprusside (SNP) induced an increase of the cytosolic calcium concentration (...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.05.009

    authors: Pan L,Song K,Hu F,Sun W,Lee I

    更新日期:2013-09-05 00:00:00

  • Effects of proglumetacin maleate and its major metabolites on allergic air pouch inflammation in rats.

    abstract::The mechanism of the anti-inflammatory effect of proglumetacin maleate, a novel indomethacin derivative, was examined in vivo in an allergic air pouch inflammation model in rats. Proglumetacin maleate did not affect the volume of pouch exudate 6 h after immunological challenge, irrespective of whether it was administe...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90113-0

    authors: Ono N,Sunami A,Yamasaki Y,Yamamoto N,Miyake H

    更新日期:1987-10-13 00:00:00

  • A comparative study of alpha-adrenergic receptor mediated Ca(2+) signals and contraction in intact human and mouse vascular smooth muscle.

    abstract::In many vascular smooth muscle cells, physiological and pharmacological agonists initiate oscillatory fluctuations in intracellular Ca(2+) to initiate and maintain vasoconstriction. These oscillations are supported by the underlying cellular ultrastructure, particularly the close apposition between the plasma membrane...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.11.055

    authors: Dai JM,Syyong H,Navarro-Dorado J,Redondo S,Alonso M,van Breemen C,Tejerina T

    更新日期:2010-03-10 00:00:00

  • Haemodynamic effects of vasoactive agents following chronic state of high cardiac output in anaesthetized rats.

    abstract::The arteriovenous fistula model of circulation can produce a high output and low peripheral resistance situation. Here, we have examined the effects of noradrenaline, vasopressin and sodium nitroprusside on cardiac index, mean arterial blood pressure, venous tone, resistance to venous return, arterial resistance, and ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.02.045

    authors: Guo L,Tabrizchi R

    更新日期:2008-05-31 00:00:00

  • Current knowledge and pharmacological profile of berberine: An update.

    abstract::Berberine, a benzylisoquinoline alkaloid, occurs as an active constituent in numerous medicinal plants and has an array of pharmacological properties. It has been used in Ayurvedic and Chinese medicine for its antimicrobial, antiprotozoal, antidiarrheal and antitrachoma activity. Moreover, several clinical and preclin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2015.05.068

    authors: Kumar A,Ekavali,Chopra K,Mukherjee M,Pottabathini R,Dhull DK

    更新日期:2015-08-15 00:00:00

  • Reduction of a centrally induced pressor response by neurohypophyseal peptides: the involvement of lower brainstem mechanisms.

    abstract::Pressor and bradycardiac responses induced by electrical stimulation of the mesencephalic reticular formation in urethane-anesthetized rats were used as model of neurogenic hypertension. Oxytocin (OXT) and prolyl-leucyl-glycinamide (OXT-(7-9] administered into the fourth cerebral ventricle markedly attenuated the magn...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90450-8

    authors: Versteeg CA,Cransberg K,De Jong W,Bohus B

    更新日期:1983-10-14 00:00:00

  • Further studies on ocular responses to DP receptor stimulation.

    abstract::Prostaglandin D2 (PGD2) and the selective DP receptor agonist BW 245C have been previously shown to lower intraocular pressure in rabbits, while PGD2, but not BW 245C, caused plasma extravasation, eosinophil infiltration, and goblet cell depletion. In these present studies definition of the ocular pharmacology of pros...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90569-4

    authors: Woodward DF,Spada CS,Hawley SB,Williams LS,Protzman CE,Nieves AL

    更新日期:1993-01-19 00:00:00

  • Potentiation by neuropeptide Y of 5HT2A receptor-mediated contraction in porcine coronary artery.

    abstract::Potentiation by neuropeptide Y of serotonin (5-HT)-induced vasoconstriction was investigated in porcine coronary artery. 5-HT caused concentration-dependent contraction through 5-HT2A receptors. Neuropeptide Y (30 nM) significantly increased the 5HT-induced contraction by 16+/-5% in arteries with intact endothelium. R...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.06.036

    authors: Tsurumaki T,Nagai S,Bo X,Toyosato A,Higuchi H

    更新日期:2006-08-21 00:00:00

  • L-Arginine supplementation improves insulin sensitivity and beta cell function in the offspring of diabetic rats through AKT and PDX-1 activation.

    abstract::Maternal hyperglycemia can result in defects in glucose metabolism and pancreatic β-cell function in offspring. The purpose of this study was to evaluate the impact of maternal diabetes mellitus on pancreatic islets, muscle and adipose tissue of the offspring, with or without oral l-Arginine supplementation. The induc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.10.001

    authors: Carvalho DS,Diniz MM,Haidar AA,Cavanal MF,da Silva Alves E,Carpinelli AR,Gil FZ,Hirata AE

    更新日期:2016-11-15 00:00:00

  • Cav3.2 overexpression in L4 dorsal root ganglion neurons after L5 spinal nerve cutting involves Egr-1, USP5 and HMGB1 in rats: An emerging signaling pathway for neuropathic pain.

    abstract::Overexpression of Cav3.2 T-type Ca2+ channels in L4 dorsal root ganglion (DRG) participates in neuropathic pain after L5 spinal nerve cutting (L5SNC) in rats. The L5SNC-induced neuropathic pain also involves high mobility group box 1 (HMGB1), a damage-associated molecular pattern protein, and its target, the receptor ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173587

    authors: Tomita S,Sekiguchi F,Kasanami Y,Naoe K,Tsubota M,Wake H,Nishibori M,Kawabata A

    更新日期:2020-12-05 00:00:00

  • Discriminative stimulus properties of physostigmine in rats.

    abstract::Sprague-Dawley rats were trained to discriminate a subcutaneous injection of physostigmine (0.2 mg/kg) from a similar injection of saline in a two-lever, food-reinforced behavior paradigm. The training dose of physostigmine reduced the response rate to about 50% of that in saline sessions. The discriminative stimulus ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90592-4

    authors: Tang AH,Franklin SR

    更新日期:1988-08-09 00:00:00

  • Isobolographic analysis of interactions between 1-methyl-1,2,3,4-tetrahydroisoquinoline and four conventional antiepileptic drugs in the mouse maximal electroshock-induced seizure model.

    abstract::The anticonvulsant activity of 1-methyl-1,2,3,4-tetrahydroisoquinoline (MeTHIQ--an endogenous parkinsonism-preventing substance) administered alone and in combination with four conventional antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and valproate) was determined in the mouse maximal electroshock-indu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.11.049

    authors: Luszczki JJ,Antkiewicz-Michaluk L,Czuczwar SJ

    更新日期:2009-01-14 00:00:00

  • Inhibition by antipsychotic drugs of L-type Ca2+ channel current in PC12 cells.

    abstract::Inhibition by antipsychotic drugs of voltage-gated L-type Ca2+ channels was characterized in rat neuronal cell line pheochromocytoma PC12 cells. Under whole-cell voltage-clamp, haloperidol and chlorpromazine (1-100 microM) inhibited Ba2+ current permeating through Ca2+ channels. Fluspirilene and pimozide the Ba2+ curr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(96)00500-6

    authors: Ito K,Nakazawa K,Koizumi S,Liu M,Takeuchi K,Hashimoto T,Ohno Y,Inoue K

    更新日期:1996-10-24 00:00:00

  • Tanshinone ⅡA inhibits VSMC inflammation and proliferation in vivo and in vitro by downregulating miR-712-5p expression.

    abstract::The inflammation and proliferation of vascular smooth muscle cells (VSMCs) are the basic pathological feature of proliferative vascular diseases. Tanshinone ⅡA (Tan ⅡA), which is the most abundant fat-soluble element extracted from Salvia miltiorrhiza, has potent protective effects on the cardiovascular system. Howeve...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173140

    authors: Qin Y,Zheng B,Yang GS,Zhou J,Yang HJ,Nie ZY,Wang TR,Zhang XH,Zhao HY,Shi JH,Wen JK

    更新日期:2020-08-05 00:00:00

  • The alpha and gamma subunit-dependent effects of local anesthetics on recombinant GABA(A) receptors.

    abstract::Although convulsions due to local anesthetic systemic toxicity are thought to be due to inhibition of GABA(A) receptor-linked currents in the central nervous system, the mechanism of action remains unclear. We therefore examined the effects of local anesthetics on gamma-aminobutyric acid (GABA)-induced currents using ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00463-5

    authors: Sugimoto M,Uchida I,Fukami S,Takenoshita M,Mashimo T,Yoshiya I

    更新日期:2000-08-11 00:00:00

  • Analysis of the antinociceptive interactions in two-drug combinations of gabapentin, oxcarbazepine and amitriptyline in streptozotocin-induced diabetic mice.

    abstract::Antiepileptic and antidepressant drugs are the primary treatments for pain relief in diabetic neuropathy. Combination therapy is a valid approach in pain treatment, where a reduction of doses could reduce side effects and still achieve optimal analgesia. We examined the effects of two-drug combinations of gabapentin, ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.11.016

    authors: Tomić MA,Vucković SM,Stepanović-Petrović RM,Micov AM,Ugresić ND,Prostran MS,Bosković B

    更新日期:2010-02-25 00:00:00

  • Role of vagal afferents in the antinociception produced by morphine and U-50,488H in the colonic pain reflex in rats.

    abstract::The mechanisms underlying the antinociception induced by morphine or U-50,488H (trans-(+-)-3,4-dichloro-N-methyl-N-(2-[1-pyrrolidinyl]- cyclohexyl)benzeneacetamide) against painful colonic distension were examined in anaesthetized rats. The respective ED50 values for morphine and U-50,488H were 0.34 and 0.35 mg/kg for...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90710-2

    authors: Diop L,Rivière PJ,Pascaud X,Dassaud M,Junien JL

    更新日期:1994-05-12 00:00:00

  • Correlation between neuroleptic binding to sigma(1) and sigma(2) receptors and acute dystonic reactions.

    abstract::Acute dystonic reactions are motor side effects that occur soon after the initiation of neuroleptic treatment. Although earlier studies indicate that these abnormal movements can be induced in animals and humans via activation of sigma receptors, the relative contribution of the different sigma receptor subtypes is un...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00430-1

    authors: Matsumoto RR,Pouw B

    更新日期:2000-08-04 00:00:00

  • A comparison of the abilities of typical neuroleptic agents and of thioridazine, clozapine, sulpiride and metoclopramide to antagonise the hyperactivity induced by dopamine applied intracerebrally to areas of the extrapyramidal and mesolimbic systems.

    abstract::Dopamine injected directly into the caudate--putamen, nucleus accumbens or tuberculum olfactorium of rat brain, following a nialamide pretreatment, caused dose-dependent hyperactivity. The hyperactivity was more intense after injections into the nucleus accumbens, but was limited by the development of stereotyped biti...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(76)90348-4

    authors: Costall B,Naylor RJ

    更新日期:1976-11-01 00:00:00

  • The mechanism of apoptosis induced by a novel thioredoxin reductase inhibitor in A549 cells: possible involvement of nuclear factor-kappaB-dependent pathway.

    abstract::1,2-[bis(1,2-benzisoselenazolone-3(2H)-ketone)]ethane (BBSKE, PCT: CN02/00412), a novel thioredoxin reductase inhibitor previously synthesized in our lab, has been demonstrated to inhibit the growth of a variety of human cancer cells and to induce apoptosis. Here we report on the potential molecular mechanism of apopt...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.10.037

    authors: Lan L,Zhao F,Wang Y,Zeng H

    更新日期:2007-01-26 00:00:00

  • Anxiolytic activity on locus coeruleus-mediated suppression of muricidal aggression.

    abstract::The evidence suggests that stimulation of brain noradrenergic neurons plays an inhibitory role in rat mouse-killing (muricidal) aggression. Anxiolytic benzodiazepines inhibit locus coeruleus activity and previous data showed that chlordiazepoxide was capable of antagonizing the locus coeruleus-mediated suppression of ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90625-3

    authors: Kozak W,Valzelli L,Garattini S

    更新日期:1984-10-15 00:00:00

  • Interaction of sulfonylureas with the transport of bile acids into hepatocytes.

    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

    authors: Fückel D,Petzinger E

    更新日期:1992-03-31 00:00:00

  • Comparison of short-term administration of sertindole, clozapine and haloperidol on the inactivation of midbrain dopamine neurons in the rat.

    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

    authors: Skarsfeldt T

    更新日期:1994-03-21 00:00:00