Evidence for a 5-HT1D receptor-mediated hypothermic effect of the alpha 1-adrenoceptor agonist, SDZ NVI-085, in guinea-pigs.

Abstract:

:The alpha 1-adrenoceptor agonist, SDZ NVI-085 ((-)-(4aR,10aR)-3,4,4a,5,10,10a-hexahydro-6-methoxy-4- methyl-9-(methylthio)-2H-naphth[2,3-b]-1,4-oxazine.HCl; 1 mg/kg i.p.), decreased body temperature of guinea-pigs. Two 5-HT1D receptor antagonists, GR127935 (N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(5-methyl- 1,2,4-oxadiazol-3yl)[1,1-biphenyl]-4-carboxamide) and PAPP (p-aminophenylethyl-m-trifluoromethylphenyl piperazine; both compounds at 1 mg/kg i.p., -30 min) blocked this response, whilst the alpha 1-adrenoceptor blocker prazosin (1 mg/kg i.p.) and the 5-HT1A receptor antagonist, SDZ 216-525 (methyl 4-(-[4-(1,1m3-trioxo-2H-1,2-benzoisothiazol-2-yl)butyl ]-1-piperazinyl)1H- indole-2-carboxylate; 1 mg/kg i.p.) were inactive. Another alpha 1-adrenoceptor agonist, St 587 (2-(2-chloro-5-trifluoromethylphenylimino)-imidazoline; 1 mg/kg i.p.) did not alter body temperature. SDZ NVI-085-induced hypothermia in guinea-pigs is probably mediated by 5-HT1D receptors.

journal_name

Eur J Pharmacol

authors

Kalkman HO,Neumann V

doi

10.1016/0014-2999(95)00526-q

subject

Has Abstract

pub_date

1995-10-24 00:00:00

pages

313-5

issue

3

eissn

0014-2999

issn

1879-0712

pii

001429999500526Q

journal_volume

285

pub_type

杂志文章
  • L-type calcium channels contribute to 5-HT3-receptor-evoked CaMKIIα and ERK activation and induction of emesis in the least shrew (Cryptotis parva).

    abstract::Activation of serotonergic 5-HT3 receptors by its selective agonist 2-methyl serotonin (2-Me-5-HT) induces vomiting, which is sensitive to selective antagonists of both 5-HT3 receptors (palonosetron) and L-type calcium channels (LTCC) (amlodipine or nifedipine). Previously we demonstrated that 5-HT3 receptor activatio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2015.02.042

    authors: Hutchinson TE,Zhong W,Chebolu S,Wilson SM,Darmani NA

    更新日期:2015-05-15 00:00:00

  • Studies on the role of 5-HT2C and 5-HT2B receptors in regulating generalised seizure threshold in rodents.

    abstract::The present studies were conducted to investigate the role of 5-HT2C and 5-HT2B receptors in the generation of pentylenetetrazol and electroshock-evoked seizures. The 5-HT2C/2B receptor-preferring agonist 1-(m-chlorophenyl)-piperazine (mCPP; 2.5-7 mg/kg i.p.) weakly elevated seizure threshold in the mouse (but not the...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00621-9

    authors: Upton N,Stean T,Middlemiss D,Blackburn T,Kennett G

    更新日期:1998-10-16 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

  • The role of alpha 1-adrenoceptor subtypes in the regulation of arterial blood pressure.

    abstract::The effect of chlorethylclonidine on alpha 1-adrenoceptor subtypes and arterial blood pressure has been evaluated. Chlorethylclonidine significantly reduced the alpha 1-adrenoceptor population. Chlorethylclonidine treatment had no significant effect on resting systemic arterial blood pressure or heart rate and shifted...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90327-3

    authors: Piascik MT,Butler BT,Pruitt TA

    更新日期:1990-05-16 00:00:00

  • Ethyl beta-carboline-3-carboxylate reverses the diazepam effect on cerebellar cyclic GMP.

    abstract::The administration of ethyl beta-carboline-3-carboxylate (beta-CCE), a ligand for benzodiazepine receptors, did not affect the cerebellar cyclic GMP level in mice, but giving beta-CCE together with diazepam significantly inhibited the diazepam-induced decrease in cyclic GMP. The fact that no antagonism was observed wh...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90065-6

    authors: Fujimoto M,Kawasaki K,Matsushita A,Okabayashi T

    更新日期:1982-05-21 00:00:00

  • Protein kinase A-dependent coupling of mouse prostacyclin receptors to Gi is cell-type dependent.

    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

    authors: Chow KB,Jones RL,Wise H

    更新日期:2003-08-01 00:00:00

  • Stimulant effect of the beta-carboline FG 7142 in the open-field test.

    abstract::The anxiogenic activity of N-methyl-beta-carboline-3-carboxamide (FG 7142) is sometimes difficult to observe in rats. As the open field has recently been applied successfully to test the anxiogenic potential of n-butyl-beta-carboline-3-carboxylate (beta-CCB) in mice, a comparable experiment was performed with FG 7142 ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90685-j

    authors: Bruhwyler J,Chleide E,Houbeau G,Mercier M

    更新日期:1991-07-23 00:00:00

  • The genetic deletion of Mas abolishes salt induced hypertension in mice.

    abstract::The G protein-coupled receptor Mas is a physiological antagonist of the angiotensin II type 1 receptor and is associated with angiotensin-(1-7) signaling. We investigated the effect of Mas-deficiency on blood pressure regulation under physiological conditions and salt load using radiotelemetry. Mas-knockout mice and t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.05.025

    authors: Heringer-Walther S,Gembardt F,Perschel FH,Katz N,Schultheiss HP,Walther T

    更新日期:2012-08-15 00:00:00

  • Potentiation by metal ions of ryanodine contracture of the mouse diaphragm.

    abstract::The aim of this study was to elucidate the possible mechanism of the potentiating action of metal ions (Cu2+, Hg2+, Ag+ and SeO3(2-)) on the ryanodine-induced contracture of the mouse diaphragm. The ryanodine contracture in the quiescent muscle could be augmented by either electrical stimulation or pretreatment with h...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90443-x

    authors: Liu SH,Lin-Shiau SY

    更新日期:1994-01-04 00:00:00

  • Paeoniflorin inhibits imiquimod-induced psoriasis in mice by regulating Th17 cell response and cytokine secretion.

    abstract::Paeoniflorin (PF) is the main active ingredients of radix paeoniae rubra and radix paeoniae alba, which are used widely in Traditional Chinese Medicine. This study aimed to assess the capacity of PF to inhibit imiquimod (IMQ)-induced psoriasis. Mice treated with IMQ were divided into four groups and administered 240mg...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2015.12.040

    authors: Zhao J,Di T,Wang Y,Wang Y,Liu X,Liang D,Li P

    更新日期:2016-02-05 00:00:00

  • Resveratrol provides late-phase cardioprotection by means of a nitric oxide- and adenosine-mediated mechanism.

    abstract::We used two experimental models to prove that resveratrol (trans-3,4',5-trihydroxystilbene) reduces cardiac ischemic-reperfusion injury by means of a nitric oxide- and adenosine-dependent mechanism. (1). ACUTE EX VIVO: resveratrol (10 microM, 10 min) infusion in Langendorff-perfused normoxic rat hearts significantly i...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)01441-9

    authors: Bradamante S,Barenghi L,Piccinini F,Bertelli AA,De Jonge R,Beemster P,De Jong JW

    更新日期:2003-03-28 00:00:00

  • Voltage-dependent action of valproate on potassium channels in frog node of Ranvier.

    abstract::The influence of the anti-epileptic drug, valproate, on K conductance (gK) was investigated in voltage-clamped Ranvier nodes of Xenopus laevis. A double pulse method was used in order to eliminate the effect of accumulation of potassium ions in the perinodal space, thus enabling the determination of the 'true' magnitu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90676-w

    authors: Van Erp MG,Van Dongen AM,Van den Berg RJ

    更新日期:1990-08-02 00:00:00

  • TFMPP and RU24969 enhance serotonin release from rat hippocampus.

    abstract::Using a batch method for incubation of hippocampal slices, we have examined the effects of 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole (RU24969) and (m-trifluoromethylphenyl)piperazine (TFMPP) on release of endogenous 5-hydroxytryotamine (5-HT). Release of 5-HT from slices was enhanced by RU24969 and TFMPP ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)94111-a

    authors: Auerbach SB,Kamalakannan N,Rutter JJ

    更新日期:1990-11-06 00:00:00

  • Low-dose hydralazine improves endotoxin-induced coagulopathy and multiple organ dysfunction via its anti-inflammatory and anti-oxidative/nitrosative properties.

    abstract::Coagulopathy is the major cause of organ injury as well as a strong predictor of mortality in septic patients. Systemic inflammatory response and redox imbalance are regarded as the major causes of sepsis-induced coagulopathy. There is growing evidence that a vasodilator hydralazine has beneficial effects on heart fai...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173279

    authors: Huang HC,Hsiao TS,Liao MH,Tsao CM,Shih CC,Wu CC

    更新日期:2020-09-05 00:00:00

  • Effects of seganserin, a 5-HT2 antagonist, and temazepam on human sleep stages and EEG power spectra.

    abstract::The effects of seganserin, a specific 5HT2 antagonist, on human sleep were assessed in two experiments and compared to the effects of temazepam and sleep deprivation. During daytime recovery sleep after sleep deprivation, seganserin did not significantly enhance visually scored slow wave sleep (SWS, stages 3 + 4) or t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90109-x

    authors: Dijk DJ,Beersma DG,Daan S,van den Hoofdakker RH

    更新日期:1989-11-21 00:00:00

  • Effects of FK409, a nitric oxide donor, on renal responses to renal nerve stimulation in anesthetized dogs.

    abstract::We examined the effects of (+/-)-(E)-4-ethyl-2-[(E)-hydroxyimino]-5-nitro-3-hexenamide (FK409), a nitric oxide (NO) donor, on renal actions and norepinephrine overflow induced by renal nerve stimulation in anesthetized dogs, with or without N(G)-nitro-L-arginine (NOARG), a NO synthase inhibitor. Renal nerve stimulatio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)01424-6

    authors: Tadano K,Matsuo G,Hashimoto T,Matsumura Y

    更新日期:1998-01-12 00:00:00

  • Cyclosporin A targets involved in protection against glutamate excitotoxicity.

    abstract::The toxicity of glutamate in neuronal cultures has been attributed in part to a mitochondrial dysfunction involving the permeability transition pore. The participation of the permeability transition pore in this process has been pharmacologically demonstrated by the use of cyclosporin A, which inhibits pore opening by...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00584-7

    authors: Ruiz F,Alvarez G,Ramos M,Hernández M,Bogónez E,Satrústegui J

    更新日期:2000-09-15 00:00:00

  • Effects of chlorpromazine and some of its metabolites on the EEG and on dopamine metabolism of the isolated perfused rat brain.

    abstract::The study concerned the effects of chlorpromazine (CPZ), monodesmethyl-chlorpromazine (NOR1-CPZ), didesmethyl-chlorpromazine (NOR2-CPZ), and chlorpromazine-N-oxide (CPZ-NO) on the EEG and on dopamine metabolism of the isolated perfused rat brain. Isolated brains were perfused with 100 ml of a perfusion medium containi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(79)90267-x

    authors: Krieglstein J,Rieger H,Schütz H

    更新日期:1979-07-01 00:00:00

  • The anxiolytics CI-988 and chlordiazepoxide fail to reduce immediate early gene mRNA stimulation following exposure to the rat elevated X-maze.

    abstract::This study uses immediate early transcription factor gene expression to map neuronal activation after a single exposure to the elevated X-maze. Exposure to this novel environment leads to widespread upregulation in the gene expression of c-fos, NGFI-A and NGFI-B (the nerve growth factor induced genes), but not c-jun n...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(96)00471-2

    authors: Hinks GL,Brown P,Field M,Poat JA,Hughes J

    更新日期:1996-09-26 00:00:00

  • Beneficial effect of pharmacological mobilization of bone marrow in experimental cerebral ischemia.

    abstract::Bone marrow stem cells are able to differentiate into nervous and endothelial cells. In our study, we found that administration of a bone marrow-stimulating factor (granulocyte colony-stimulating factor; G-CSF 50 microg/kg) decrease the brain infarct volume and enhance survival rate in a model of cerebral ischemia. Ta...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)02785-1

    authors: Six I,Gasan G,Mura E,Bordet R

    更新日期:2003-01-05 00:00:00

  • Co-administration of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid and arachidonic acid potentiates synaptic transmission in rat hippocampal slices.

    abstract::Perfusion of the 1S,3R isomer of trans-aminocyclopentane-1,3-dicarboxylic acid (t-ACPD, 50 microM), or arachidonic acid (10 microM), for 5 min produced only depression of the field excitatory postsynaptic potential recorded in the CA1 region of rat hippocampal slices from which the CA3 region had been removed. However...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90919-9

    authors: Collins DR,Davies SN

    更新日期:1993-08-24 00:00:00

  • Cytoskeletal interference - A new mode of action for the anticancer drugs camptothecin and topotecan.

    abstract::The anticancer drugs camptothecin (CPT) and topotecan (TPT) are known DNA topoisomerase I inhibitors which cause DNA damage and lead to cell death. In this study we provide evidence that CPT and TPT also interfere with the elements of cytoskeleton - microtubules and actin filaments which could be partly responsible fo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.07.044

    authors: Wang X,Tanaka M,Krstin S,Peixoto HS,Moura CCM,Wink M

    更新日期:2016-10-15 00:00:00

  • Induction of cytochrome P450 1A1 expression by ginsenoside Rg1 and Rb1 in HepG2 cells.

    abstract::Transcriptional activation of the human CYP1A1 gene (coding for cytochrome P450 1A1) is mediated by the aryl hydrocarbon receptor. In the present study we have examined interaction of the ginsenoside Rg1 and Rb1 with the carcinogen activation pathway mediated by the aryl hydrocarbon receptor in HepG2 cells. RT-PCR was...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.10.057

    authors: Wang Y,Ye X,Ma Z,Liang Q,Lu B,Tan H,Xiao C,Zhang B,Gao Y

    更新日期:2008-12-28 00:00:00

  • α1D-adrenoceptor involves the relaxation effect of farrerol in rat aortic vascular smooth muscle cells.

    abstract::The aim of this study was to investigate the relaxation effect of farrerol on rat aortic vascular smooth muscle cells (VSMCs) and its underlying mechanism. VSMCs were cultured primarily and were used to examine the relaxation effect of farrerol. Cells surface and length were measured by dynamic observation, or by rhod...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2019.02.012

    authors: Qin X,Hou X,Zhang K,Li Q

    更新日期:2019-06-15 00:00:00

  • Allosteric interactions between gamma-aminobutyric acid, benzodiazepine and picrotoxinin binding sites in primary cultures of cerebellar granule cells. Differential effects induced by gamma- and delta-hexachlorocyclohexane.

    abstract::Allosterism between gamma-aminobutyric acid (GABA), benzodiazepine and picrotoxinin recognition sites on the GABAA receptor was studied in primary cultures of cerebellar granule cells. The increase in [3H]flunitrazepam binding induced by GABA was inhibited by bicuculline and picrotoxinin and the decrease in [35S]t-but...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(96)00866-7

    authors: Vale C,Pomés A,Rodríguez-Farré E,Suñol C

    更新日期:1997-01-29 00:00:00

  • The beneficial in vitro effects of lovastatin and chelerythrine on relaxatory response to acetylcholine in the perfused mesentric bed isolated from diabetic rats.

    abstract::Diabetes mellitus is associated with an increased risk of cardiovascular disease. Endothelial dysfunction (i.e. decreased endothelium-dependent vasorelaxation) plays a key role in the pathogenesis of diabetic vascular disease. The present study was undertaken to determine whether diabetes induced by streptozotocin alt...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.01.063

    authors: Fatehi-Hassanabad Z,Imen-Shahidi M,Fatehi M,Farrokhfall K,Parsaeei H

    更新日期:2006-03-27 00:00:00

  • Characterization of FR 172357, a new non-peptide bradykinin B(2) receptor antagonist, in human, pig and rabbit preparations.

    abstract::FR 172357, a new non-peptide antagonist of the kinin B(2) receptor was tested in three isolated vessels, the human umbilical vein, the rabbit jugular vein, and the pig coronary artery, to evaluate its antagonistic activities against bradykinin. FR 172357 displaced to the right the concentration-response curves of brad...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00711-6

    authors: Rizzi C,Rizzi A,Calò G,Jorizzo G,Agnello G,Mollica G,Inamura N,Regoli D

    更新日期:1999-12-10 00:00:00

  • Functional study on vasodilator effects of prostaglandin E2 in the newborn pig cerebral circulation.

    abstract::Cerebral vascular reactivity to prostaglandin E2 was investigated in newborn pigs using closed cranial windows. Exogenous prostaglandin E2 is a dilator of pial arterioles that elevates cyclic AMP in cortical cerebrospinal fluid. Pial arterioles are less sensitive to prostaglandin E2 than to the prostacyclin receptor a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00113-y

    authors: Parfenova H,Leffler CW

    更新日期:1995-05-15 00:00:00

  • Ugonin K-stimulated osteogenesis involves estrogen receptor-dependent activation of non-classical Src signaling pathway and classical pathway.

    abstract::We have reported previously that ugonin K, a flavonoid isolated from Helminthostachys zeylanica (L.) Hook, potently induces cell differentiation and mineralization of MC3T3-E1 mouse osteoblast-like cells. Here we aimed to elucidate whether ugonin K evoked osteogenesis required interaction with estrogen receptor. Resul...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.12.001

    authors: Lee CH,Huang YL,Liao JF,Chiou WF

    更新日期:2012-02-15 00:00:00

  • Anti-exudative effects of opioid receptor agonists in a rat model of carrageenan-induced acute inflammation of the paw.

    abstract::We evaluated the anti-exudative effects (Evan's blue) of mu-, delta- and kappa-opioid receptor agonists in a rat model of carrageenan-induced acute inflammation. The contribution of different components was assessed after the administration of: cyclosporine A, capsaicin, 6-hydroxydopamine, compound 48/80, and specific...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.02.004

    authors: Romero A,Planas E,Poveda R,Sánchez S,Pol O,Puig MM

    更新日期:2005-03-28 00:00:00