GABAA and GABAB receptors in locus coeruleus: effects of blockers.

Abstract:

:Racemic baclofen, (-)-baclofen and muscimol depressed all spontaneously firing locus coeruleus neurons tested in a slice preparation. Racemic phaclofen (100 microM; 1 mM) moderately antagonized the effects of racemic baclofen without antagonizing those of muscimol. Bicuculline (10, 30, 100 microM) potently antagonized the action of muscimol without affecting the inhibition of baclofen. Phaclofen and bicuculline had no pronounced effect on the spontaneous discharge rate of cells. The results suggests that there are GABAA and GABAB receptors in the locus coeruleus.

journal_name

Eur J Pharmacol

authors

Olpe HR,Steinmann MW,Hall RG,Brugger F,Pozza MF

doi

10.1016/0014-2999(88)90061-1

subject

Has Abstract

pub_date

1988-04-27 00:00:00

pages

183-5

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(88)90061-1

journal_volume

149

pub_type

杂志文章
  • Pharmacokinetic-pharmacodynamic influence of N-palmitoylethanolamine, arachidonyl-2'-chloroethylamide and WIN 55,212-2 on the anticonvulsant activity of antiepileptic drugs against audiogenic seizures in DBA/2 mice.

    abstract::We evaluated the effects of ACEA (selective cannabinoid (CB)1 receptor agonist), WIN 55,212-2 mesylate (WIN; non-selective CB1 and CB2 receptor agonist) and N-palmitoylethanolamine (PEA; an endogenous fatty acid of ethanolamide) in DBA/2 mice, a genetic model of reflex audiogenic epilepsy. PEA, ACEA or WIN intraperito...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.09.029

    authors: Citraro R,Russo E,Leo A,Russo R,Avagliano C,Navarra M,Calignano A,De Sarro G

    更新日期:2016-11-15 00:00:00

  • Two dopamine receptors: supportive evidence with the rat rotational model.

    abstract::Di-isobutyryl apomorphine (5 mg/kg i.p.) and lergotrile (5 mg/kg i.p.) produce long lasting turning behaviour in rats with 6-hydroxydopamine lesions at the level of the substantia nigra. Haloperidol (1.5 and 3.0 mg/kg p.o.) blocks the rotational behaviour due to the apomorphine ester but has no effect on lergotrile tu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(77)90063-2

    authors: Tye NC,Horsman L,Wright FC,Large BT,Pullar IA

    更新日期:1977-09-01 00:00:00

  • Antinociceptive studies of the optical isomers of N-allylnormetazocine (SKF 10,047).

    abstract::In the mouse tail-flick test, neither the racemate of N-allylnormetazocine (NANM) nor its optical isomers showed antinociceptive activity. However, all three antagonized morphine's tail-flick effects. In the phenylquinone test in mice, the racemate and (-)-isomer of NANM showed agonist activity and antagonized morphin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90476-4

    authors: Aceto MD,May EL

    更新日期:1983-07-22 00:00:00

  • Curcumol exhibits anti-inflammatory properties by interfering with the JNK-mediated AP-1 pathway in lipopolysaccharide-activated RAW264.7 cells.

    abstract::Curcumol is one of the major components of the essential oil of Rhizoma Curcumae, a common traditional Chinese medicine with anti-inflammatory properties. However, the anti-inflammatory activity and the underlying molecular mechanisms of this compound remain unclear. In the present study, the anti-inflammation effect ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.11.007

    authors: Chen X,Zong C,Gao Y,Cai R,Fang L,Lu J,Liu F,Qi Y

    更新日期:2014-01-15 00:00:00

  • Dopamine agonist-induced hyperglycemia in rats: structure-activity relationships and mechanisms of action.

    abstract::The concentration of blood glucose was measured in rats after administration of a number of drugs characterized as dopamine agonists. Compounds that cause release of dopamine, or agents that block the reuptake of dopamine, did not elevate blood glucose. Some direct dopamine receptor stimulants (lergotrile, bromocripti...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90234-0

    authors: Schmidt MJ,Root MA,Hall JL

    更新日期:1983-06-03 00:00:00

  • [3H]Batrachotoxinin A 20-alpha-benzoate binding to sodium channels in rat brain: characterization and pharmacological significance.

    abstract::Attempts were made to find whether [3H]batrachotoxinin A 20-alpha-benzoate provides a specific probe for measuring interactions of local anesthetics with the sodium channel complex. [3H]Batrachotoxinin A 20-alpha-benzoate binding, [14C]guanidine and 22Na uptake were investigated in rat brain crude synaptosomal prepara...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90230-x

    authors: Pauwels PJ,Leysen JE,Laduron PM

    更新日期:1986-05-27 00:00:00

  • The effect of Bay K 8644 on angiotensin II-induced contractions of rabbit aortic strips.

    abstract::The effect of Bay K 8644 on contractile responses to angiotensin II (AII) was investigated in rabbit aorta. Bay K 8644 alone did not elicit contraction while contractile responses to AII were enhanced at low concentrations (10(-8), 3 X 10(-8), 10(-7) M) and depressed at a higher concentration (10(-6) M). The potentiat...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90755-7

    authors: Roy F,Pruneau D

    更新日期:1986-07-15 00:00:00

  • A comparative study in rats of the respiratory depression and analgesia induced by mu- and delta-opioid agonists.

    abstract::A comparison was made in awake rats between the analgesic and the respiratory depressant actions induced by the mu-opiate agonists morphine and Tyr-D-Ala-Gly-N-Me-Phe-Met-(O)-ol (FK-33824), and the delta-agonists Tyr-D-Ala-Gly-Phe-D-Leu ( DADLE ) and Tyr-D-Ser-Gly-Phe-D-Leu-Thr (D-Ser2- Thr6 ), injected into the cereb...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90427-8

    authors: Pazos A,Flórez J

    更新日期:1984-03-16 00:00:00

  • Effects of glutamate-related drugs on marble-burying behavior in mice: implications for obsessive-compulsive disorder.

    abstract::Clinical evidence demonstrates altered glutamatergic neurotransmission in patients suffering from obsessive-compulsive disorder (OCD). We examined the effects of glutamate-related drugs on marble-burying behavior, which is an animal model of OCD. The uncompetitive N-methyl-d-aspartate (NMDA) antagonists memantine (10 ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.01.035

    authors: Egashira N,Okuno R,Harada S,Matsushita M,Mishima K,Iwasaki K,Nishimura R,Oishi R,Fujiwara M

    更新日期:2008-05-31 00:00:00

  • The behavioural effects of pramipexole, a novel dopamine receptor agonist.

    abstract::Pramipexole (SND 919; 2-amino-4,5,6,7-tetrahydro-6-propyl-amino-benzthiazole-dihydroc hlo ride) is a novel dopamine D2 family receptor agonist with a predominant action on D2 autoreceptors and with some D3 vs. D2 receptor preference. The central behavioural effects of pramipexole given subcutaneously to rats (male Wis...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)00066-6

    authors: Maj J,Rogóz Z,Skuza G,Kołodziejczyk K

    更新日期:1997-04-11 00:00:00

  • Mechanisms underlying the inhibitory effect of dibutyryl cyclic AMP in vascular smooth muscle.

    abstract::The mechanism by which dibutyryl cyclic AMP (db-cAMP) induces vasodilatation was examined in isolated rat aorta. The contraction induced by norepinephrine (NE) was more sensitive to the inhibitory effect of db-cAMP than that induced by high K+, and the contraction induced by lower concentrations of each stimulant was ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90385-h

    authors: Abe A,Karaki H

    更新日期:1992-02-18 00:00:00

  • Effect of local bleomycin sulfate application on seroma formation in a rat mastectomy and axillary lymph node dissection model.

    abstract::Seroma formation is one of the most common complications following breast cancer surgery. It may lead to delay of adjuvant therapies and increasement of therapy costs. Bleomycin sulfate is a sclerosing antibiotic with antineoplastic efficacy. It is locally used in the treatment of pleural effusion. The present study a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.10.067

    authors: Eser M,Gökçeimam M,Eyvaz K,Tutal F,Geçer MÖ,Göktaş S,Uzun H,Kaptanoglu L,Kurt N

    更新日期:2014-01-15 00:00:00

  • Identification of subtypes of [3H]prazosin-labelled alpha 1 receptor binding sites in rat brain.

    abstract::Detailed antagonist competition curves for [3H]prazosin-labelled binding sites in rat cerebral cortex membranes reveal anomalous binding characteristics. Dihydroergocryptine and indoramine compete in a steep, monophasic manner while WB4101 and phentolamine exhibit shallow competition curves. Computer-assisted analysis...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90432-7

    authors: Morrow AL,Battaglia G,Norman AB,Creese I

    更新日期:1985-02-26 00:00:00

  • Autoradiographic analysis of receptors on vascular endothelium.

    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

    authors: Stephenson JA,Summers RJ

    更新日期:1987-01-28 00:00:00

  • Endogenous nitric oxide counteracts antigen-induced bronchoconstriction.

    abstract::In anesthetized, artificially ventilated guinea pigs immunized against ovalbumin, challenge with aerosolized ovalbumin (0.1 mg) elicited a substantial and sustained increase of insufflation pressure. The inhibitor of endogenous nitric oxide (NO) synthesis, L-NAME (N omega-nitro-L-arginine methylester, 30 mg kg-1 i.v.)...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90532-m

    authors: Persson MG,Friberg SG,Hedqvist P,Gustafsson LE

    更新日期:1993-11-16 00:00:00

  • Anticholinergic agents in asthma and COPD.

    abstract::Anticholinergic agents have important uses as bronchodilators for the treatment of obstructive airway diseases, both asthma and, more particularly, chronic obstructive pulmonary disease (COPD). Those in approved clinical use are synthetic quaternary ammonium congeners of atropine, and include ipratropium bromide, oxit...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2005.12.072

    authors: Gross NJ

    更新日期:2006-03-08 00:00:00

  • Vasorelaxant mechanism of the new vasodilator, FK409.

    abstract::To define the vasorelaxation mechanism of FK409, we examined the effect of the compound on vascular tension and cyclic nucleotide levels in isolated rat thoracic aorta contracted with norepinephrine, and on activities of guanylate cyclase and cyclic GMP phosphodiesterase prepared from rat or rabbit thoracic aorta. FK4...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(93)90032-5

    authors: Isono T,Koibuchi Y,Sato N,Furuichi A,Nishii M,Yamamoto T,Mori J,Kohsaka M,Ohtsuka M

    更新日期:1993-08-15 00:00:00

  • Conditioned taste aversion: modulation by 5-HT receptor activity and corticosterone.

    abstract::Two experiments were designed to elucidate the involvement of the hypothalamic-pituitary-adrenal axis and the 5-hydroxytryptamine (5-HT) system in the acquisition of lithium chloride-conditioned taste aversion. In Experiment 1, rats were administered either vehicle or 50 mg/kg nefazodone daily for 4 weeks. Rats were t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)01790-4

    authors: Gorzalka B,Hanson L,Harrington J,Killam S,Campbell-Meiklejohn D

    更新日期:2003-06-20 00:00:00

  • Binding sites for [3H]tetracaine in synaptosomal sodium channel preparations from mouse brain.

    abstract::The present study was an attempt to answer the question whether the local anesthetic [3H]tetracaine labels sodium channels in mouse brain synaptosomes. Binding of [3H]tetracaine had a Kd of 0.19 microM and a Bmax ranging from 3.7 to 5.2 pmol/mg of protein. Local anesthetics other than tetracaine and cocaine-related co...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90530-9

    authors: Reith ME,Kim SS,Lajtha A

    更新日期:1987-11-10 00:00:00

  • The mu opiate receptor is responsible for descending pain inhibition originating in the periaqueductal gray region of the rat brain.

    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

    authors: Smith DJ,Perrotti JM,Crisp T,Cabral ME,Long JT,Scalzitti JM

    更新日期:1988-10-26 00:00:00

  • Effects of chlorogenic acid and its metabolites on the sleep-wakefulness cycle in rats.

    abstract::The effect of chlorogenic acid on the sleep-wakefulness cycle in rats was investigated in comparison with those of caffeic acid (the metabolite of chlorogenic acid) and dihydrocaffeic acid (the metabolite of caffeic acid). A significant prolongation of sleep latency was observed with chlorogenic acid and caffeic acid ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.09.054

    authors: Shinomiya K,Omichi J,Ohnishi R,Ito H,Yoshida T,Kamei C

    更新日期:2004-11-19 00:00:00

  • Tiapamil reduces the calcium inward current of isolated smooth muscle cells. Dependence on holding potential and pulse frequency.

    abstract::The calcium currents (ICa) of isolated smooth muscle cells (urinary bladder of the guinea-pig) were analyzed at 35 degrees C and 3.6 mM [Ca]0. The whole cells were voltage-clamped with a single patch electrode which was filled with 150 mM CsCl in order to block potassium outward currents. Tiapamil reduced ICa at conce...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90360-2

    authors: Klöckner U,Isenberg G

    更新日期:1986-08-15 00:00:00

  • Investigation of leukotriene involvement in the vasopermeability response associated with guinea pig tracheal anaphylaxis: comparison with cutaneous anaphylaxis.

    abstract::A direct comparison of the role of leukotrienes in mediating the increase in microvascular permeability associated with guinea pig tracheal and cutaneous anaphylaxis was obtained by simultaneous administration of inflammatory stimuli to both trachea and ear. The SRS-A antagonist, FPL 55712, reduced the increase in tra...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90025-0

    authors: Woodward DF,Wasserman MA,Weichman BM

    更新日期:1983-09-16 00:00:00

  • 2',3-dihydroxy-5-methoxybiphenyl suppresses fMLP-induced superoxide anion production and cathepsin G release by targeting the β-subunit of G-protein in human neutrophils.

    abstract::This study investigates the effect and the underlying mechanism of 2',3-dihydroxy-5-methoxybiphenyl (RIR-2), a lignan extracted from the roots of Rhaphiolepis indica (L.) Lindl. ex Ker var. tashiroi Hayata ex Matsum. & Hayata (Rosaceae), on N-formyl-L-methionyl-L-leucyl-L-phenylalanine (fMLP)-induced respiratory burst...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.03.037

    authors: Liao HR,Chen IS,Liu FC,Lin SZ,Tseng CP

    更新日期:2018-06-15 00:00:00

  • A role for endothelin ETA receptors in regulation of renal function in spontaneously hypertensive rats.

    abstract::While there is evidence to suggest that endothelin-1 is involved in regulation of kidney function and blood pressure, the importance of endothelin ETA receptors in this area has not been clearly defined. The novel, non-peptide endothelin ETA receptor antagonist, BMS-182874, (5-(dimethylamino)-N-(3,4- dimethyl-5-isoxaz...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00537-4

    authors: Bird JE,Webb ML,Giancarli MR,Chao C,Dorso CR,Asaad MM

    更新日期:1995-12-27 00:00:00

  • Decrease in endogenous CGRP release in nitroglycerin tolerance: role of ALDH-2.

    abstract::In the present study, we tested whether the decreased release of calcitonin gene-related peptide (CGRP) observed in nitroglycerin tolerance is associated with the decrease in aldehyde dehydrogenase (ALDH-2) activity. We further investigated the possible involvement of reactive oxygen species in the decrease in ALDH-2 ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.05.042

    authors: Chen YR,Nie SD,Shan W,Jiang DJ,Shi RZ,Zhou Z,Guo R,Zhang Z,Li YJ

    更新日期:2007-09-24 00:00:00

  • Aspirin and its pleiotropic application.

    abstract::Aspirin (acetylsalicylic acid), the oldest synthetic drug, was originally used as an anti-inflammatory medication. Being an irreversible inhibitor of COX (prostaglandin-endoperoxide synthase) enzymes that produce precursors for prostaglandins and thromboxanes, it has gradually found several other applications. Sometim...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2019.172762

    authors: Hybiak J,Broniarek I,Kiryczyński G,Los LD,Rosik J,Machaj F,Sławiński H,Jankowska K,Urasińska E

    更新日期:2020-01-05 00:00:00

  • Effects of 4-aminopyridine on cat blood pressure in relation to the sympathetic nervous system.

    abstract::The pressor effect of 4-aminopyridine (4-AP) was studied in anesthetized cats and in isolated cat aortic ring preparations. A significant increase in blood pressure (38.9 +/- 11.4 mmHg) was observed following intravenous administration of 4-AP (0.3 mg/kg). The elevated blood pressure lasted for 1.3 h and returned to t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90343-7

    authors: Yen MH,Lee SH,Ho ST

    更新日期:1985-07-11 00:00:00

  • Gastrins and cholecystokinins release acetylcholine but not substance P from neurons in the guinea-pig taenia coli.

    abstract::Gastrins and cholecystokinins contract the isolated taenia coli of the guinea-pig. Porcine CCK-39 produced the greatest contractile response and human gastrin-17 I and -34 the weakest. Pentagastrin had the highest affinity to the receptors and non-sulphated CCK-8 the lowest. The contractions produced by the CCK peptid...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90244-3

    authors: Nilsson S,Leander S,Vallgren S,Håkanson R

    更新日期:1983-06-03 00:00:00

  • Vagally mediated reflex and cardiac slowing induced by loperamide in rats.

    abstract::The intravenous injection of loperamide induced an immediate fall in blood pressure and heart rate in anaesthetized rats. Both effects were inhibited by the opiate antagonists naloxone and MRZ 2266 BS. Bilateral vagotomy also inhibited both effects whereas atropine only reduced the bradycardia, but the combination of ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90054-8

    authors: Gautret B,Schmitt H

    更新日期:1985-01-02 00:00:00