H1 antihistamines interact with central sigma receptors.

Abstract:

:Several antihistamines were evaluated for their ability to interact with sigma, muscarinic and histaminic H1 binding sites in rat brain preparations. All of the antihistamines were able to interact with the sigma site, as well as the other two sites. In addition, tripelennamine was found to elicit sigma-like behaviors when administered to rats. This affinity for the sigma site suggests that the compounds may elicit some of their undesirable CNS side effects via this interaction.

journal_name

Life Sci

journal_title

Life sciences

authors

Gray NM,Contreras PC,Allen SE,Taylor DP

doi

10.1016/0024-3205(90)90231-f

subject

Has Abstract

pub_date

1990-01-01 00:00:00

pages

175-80

issue

2

eissn

0024-3205

issn

1879-0631

pii

0024-3205(90)90231-F

journal_volume

47

pub_type

杂志文章
  • Effect of bilirubin on toxicity induced by trifluoperazine, dibucaine and praziquantel to erythrocytes.

    abstract::Unconjugated bilirubin (UCB), like trifluoperazine (TFP), dibucaine (DBC) and praziquantel (PZQ), induces erythrocyte morphological changes, lysis and lipid exfoliation. In the present study we determined whether TFP, DBC and PZQ toxicity to erythrocytes was potentiated or reverted by UCB. Human erythrocytes were eith...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(01)01171-7

    authors: Brito MA,Malheiros SV,Meirelles NC,Brites D

    更新日期:2001-07-13 00:00:00

  • Desensitization by cyclic AMP-dependent protein kinase of GABAB receptor expressed in Xenopus oocytes.

    abstract::Involvement of cyclic AMP-dependent protein kinase in the desensitization of GABAB receptor expressed in Xenopus oocytes was studied. GABA produced an outward current in the presence of bicuculline, under voltage-clamp conditions. Baclofen mimicked the effect of GABA, thereby indicating that the response to GABA in th...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(95)02235-1

    authors: Yoshimura M,Yoshida S,Taniyama K

    更新日期:1995-11-17 00:00:00

  • Expression of Sfrp5/Wnt5a in human epicardial adipose tissue and their relationship with coronary artery disease.

    abstract::Secreted frizzled-related protein 5 (Sfrp5) primarily acts in combination with wingless-type family member 5a (Wnt5a), to inhibits chronic inflammation and repress atherosclerosis and other metabolic disorders. Epicardial adipose tissue (EAT), surrounding the heart and coronary arteries, has been found to be highly re...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2020.117338

    authors: Tong S,Du Y,Ji Q,Dong R,Cao J,Wang Z,Li W,Zeng M,Chen H,Zhu X,Zhou Y

    更新日期:2020-03-15 00:00:00

  • Cyclic somatostatin octapeptide analogues with high affinity and selectivity toward mu opioid receptors.

    abstract::A series of cyclic conformationally restricted penicillamine containing somatostatin octapeptide analogues have been prepared by standard solid phase synthetic techniques and tested for their ability to inhibit specific [125I]CGP 23,996 (des-Ala1-,Gly2-[desamino-Cys3Tyr11]-dicarba3, 14-somatostatin), [3H]naloxone or [...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(86)90574-6

    authors: Gulya K,Pelton JT,Hruby VJ,Yamamura HI

    更新日期:1986-06-16 00:00:00

  • GnRH stimulates ACTH and immunoreactive beta-endorphin release from the rat pituitary in vitro.

    abstract::An in vitro perifusion system was used to investigate the effects of GnRH stimulation on LH, ACTH, and immunoreactive beta-endorphin (i beta-END) release from ovariectomized (1 week) rat anterior hemipituitaries. Either 0, 8 or 80 nM GnRH was administered as a 15 min pulse followed 30 min later by a prolonged 45 min i...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(88)90175-0

    authors: Gambacciani M,Yen SS,Rasmussen DD

    更新日期:1988-01-01 00:00:00

  • Effects of 1-oleoyl-2-acetyl glycerol are distinct from those of phorbol ester in rat pancreatic acini.

    abstract::1-oleoyl-2-acetyl glycerol (OAG), a potent activator of protein kinase C, inhibited the binding of 125I-labelled epidermal growth factor (EGF) in isolated rat pancreatic acini. Unlike cholecystokinin-octapeptide (CCK8) and the C-kinase activator 12-O-tetradecanoyl phorbol-13-acetate (TPA), two inhibitors of 125I-EGF e...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(87)90129-9

    authors: Brockenbrough JS,Korc M

    更新日期:1987-04-20 00:00:00

  • The responses of pulmonary and systemic circulation and airway to anaphylactic mediators in anesthetized BALB/c mice.

    abstract:AIMS:Anaphylactic shock sometimes accompanies pulmonary vaso- and broncho-constriction. We previously reported the hemodynamic features of mouse anaphylaxis (Life Sci. 2014; 116: 98-105). However, the effects of anaphylactic chemical mediators on the hemodynamics of in vivo mice are not well known. Furthermore, it is u...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2016.01.034

    authors: Wang M,Shibamoto T,Kuda Y,Tanida M,Zhang T,Song J,Kurata Y

    更新日期:2016-02-15 00:00:00

  • Estrogen dependence of the renal vasodilatory effect of nicotine in rats: role of α7 nicotinic cholinergic receptor/eNOS signaling.

    abstract:AIMS:We recently reported that acute exposure to nicotine vasodilates the renal vasculature of male rats via facilitation of endothelial nitric oxide synthase (eNOS). In this study, we investigated whether this effect of nicotine is sexually dimorphic and the role of estrogen in modulating the nicotine effect. MAIN ME...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2010.11.009

    authors: el-Mas MM,el-Gowilly SM,Gohar EY,Ghazal AR,Abdel-Rahman AA

    更新日期:2011-01-17 00:00:00

  • Thalidomide and the immune system. 2. Changes in receptors on blood cells of a healthy volunteer.

    abstract::Thalidomide (Thd) was given in two trials (total daily dose: 5 or 8 mg Thd/kg body weight, respectively) for five and three days to a healthy male volunteer, and various receptors were analyzed on white blood cells before, during and after (up to 30 days) the treatment period. There were neither marked deviations in t...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(92)90162-i

    authors: Neubert R,Nogueira AC,Neubert D

    更新日期:1992-01-01 00:00:00

  • Effects of opiates on fetal behavioral activity in utero.

    abstract::The effects of methadone and morphine on fetal behavior were studied following their administration to either the mother (5micrograms/kg/min) or fetus (0.5micrograms/kg maternal wt./min) using the chronically-instrumented pregnant ewe model. Fourteen unanesthetized, unrestrained pregnant ewes between 130-141 days gest...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(83)90584-2

    authors: Umans JG,Szeto HH

    更新日期:1983-01-01 00:00:00

  • Uptake of 131I-metaiodobenzylguanidine by 6-23 rat medullary thyroid carcinoma.

    abstract::Uptake of 131iodine-metaiodobenzylguanidine (131I-MIBG) by 6-23 rat medullary thyroid carcinoma (MTC), was studied in vitro and in vivo. In vitro, there was an 8-fold increase in 131I uptake by 6-23 cells when labeled with 131I-MIBG (131I 24 +/- 15 cpm/10(6) cells, 131I-MIBG 196 +/- 9 cpm/10(6) cells). MIBG uptake in ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(89)90456-6

    authors: Poston GJ,Fawcett HD,Townsend CM Jr,James E,Lieg JL,Nusynowitz ML,Thompson JC

    更新日期:1989-01-01 00:00:00

  • Prostaglandin E2 production by hepatic macrophages and peripheral monocytes in liver cirrhosis patients.

    abstract::We analyzed PGE2 production in primary-cultured human hepatic macrophages (HHM phi) and peripheral monocytes (MO) from patients with and without liver cirrhosis, and correlated PGE2 production with the patients' liver function. Serum choline esterase (ChE) levels were used as an indicator of liver function. PGE2 produ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(93)90751-n

    authors: Funaki N,Arii S,Adachi Y,Higashituji H,Tanaka J,Imamura M

    更新日期:1993-01-01 00:00:00

  • Dextran sulfate sodium enhances interleukin-1 beta release via activation of p38 MAPK and ERK1/2 pathways in murine peritoneal macrophages.

    abstract::Interleukin (IL)-1 beta is a pro-inflammatory cytokine that has been shown to play a pivotal role in the onset of inflammatory bowel disease (IBD), however, the molecular mechanisms underlying the production of IL-1 beta in IBD are not fully understood. We investigated dextran sulfate sodium (DSS)-induced IL-1 beta pr...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2007.05.022

    authors: Kwon KH,Ohigashi H,Murakami A

    更新日期:2007-07-12 00:00:00

  • In vivo binding of [11C]tetrabenazine to vesicular monoamine transporters in mouse brain.

    abstract::The time course of regional mouse brain distribution of radioactivity after i.v. injection of a tracer dose of [11C]tetrabenazine ([11C]TBZ) has been determined. Radiotracer uptake into brain is rapid, with 3.2% injected dose in the brain at 2 min. Egress from the brain is also very rapid, with only 0.21% of the injec...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(92)90228-h

    authors: DaSilva JN,Kilbourn MR

    更新日期:1992-01-01 00:00:00

  • Two tandem repeats of mHSP70407-426 enhance therapeutic antitumor effects of a recombined vascular endothelial growth factor (VEGF) protein vaccine.

    abstract:AIMS:Active immunization with human vascular endothelial growth factor (hVEGF) vaccines provides a therapeutic option instead of bevacizumab therapy. However, the immunity to self-molecule is difficult to elicit due to immune tolerance. A bioactive peptide of two tandem repeats of mHSP70407-426 (M2) has exhibited poten...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2018.03.039

    authors: Xu M,Zhang Y,Dong W,Jiang L,Zhang J,Yu P,Xie S,Zhou L

    更新日期:2018-05-15 00:00:00

  • Alkaline phosphatase activity during sphinganine potentiation of retinoic acid-induced differentiation of human promyelocytic leukemia cell line, HL-60.

    abstract::Sphinganine (SP) pre-treatment potentiated the retinoic acid (RA)-induced (4-96h exposures) differentiation and increase of alkaline phosphatase (ALP) activity. A higher percentage of SP pre-treated cells in RA exposures resembled mature myelocytes or granulocytes; greater increase in ALP activity was observed. In cel...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(93)90688-y

    authors: Wei LL,Hui EK,Wei JS,Tzeng WF,Yung BY

    更新日期:1993-01-01 00:00:00

  • Reactive oxygen and nitrogen species modulate the ex-vivo effects of LPS on platelet adhesion to fibrinogen.

    abstract:AIMS:Excessive production of nitric oxide (NO) and reactive oxygen species (ROS) in sepsis modulates different cell functions. Since the sepsis severity is associated with the degree of platelet activation, we decided to investigate the role of systemic generation of NO and ROS in modulating the platelet adhesion of li...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2011.09.004

    authors: Casarin AL,Lopes-Pires ME,Morganti RP,Antunes E,Marcondes S

    更新日期:2011-11-21 00:00:00

  • Ginsenoside Rg1-induced activation of astrocytes promotes functional recovery via the PI3K/Akt signaling pathway following spinal cord injury.

    abstract:AIMS:To determine whether ginsenoside Rg1 is involved in scratch wound healing through altered expression of related molecules in astrocytes and improved functional recovery after spinal cord injury (SCI). MATERIALS AND METHODS:Astrocytes were isolated from rats, followed by Rg1 treatment. The wound healing test was p...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2020.117642

    authors: Xu L,Tang YY,Ben XL,Cheng MH,Guo WX,Liu Y,Lu ZF,Deng JL

    更新日期:2020-07-01 00:00:00

  • Chronic, but not acute, administration of morphine alters antiopiate (Tyr-MIF-1) binding sites in rat brain.

    abstract::Opiate addiction could involve a change in the binding of endogenous antiopiates. A candidate for such a role is Tyr-MIF-1 (Tyr-Pro-Leu-Gly-NH2), a brain peptide that can antagonize exogenous and endogenous opiates and bind to opiate receptors. Its primary action, however, may be through its own binding site in brain,...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(89)90617-6

    authors: Zadina JE,Kastin AJ,Ge LJ,Gulden H,Bungart KJ

    更新日期:1989-01-01 00:00:00

  • Discriminative stimulus and response rate-decreasing effects of kappa opioids: antagonism by naloxone.

    abstract::The present study examined the discriminative stimulus and response rate-decreasing effects of kappa opioids in pigeons trained to discriminate a 0.017 mg/kg dose of bremazocine from saline. Bremazocine, spiradoline, CI977, U69,593 and U50,488 substituted completely for the bremazocine stimulus in a dose-dependent and...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(94)90115-5

    authors: Picker MJ

    更新日期:1994-01-01 00:00:00

  • Pre-clinical evidence for altered absorption and biliary excretion of irinotecan (CPT-11) in combination with quercetin: possible contribution of P-glycoprotein.

    abstract::P-glycoprotein (P-gp) is found to play a very significant role in intestinal and biliary transport of irinotecan and its active metabolite, SN-38. This makes P-gp inhibition a logical strategy for improving irinotecan's oral efficacy and reducing its toxicity. The objective of the present study was to identify the mos...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2008.06.007

    authors: Bansal T,Awasthi A,Jaggi M,Khar RK,Talegaonkar S

    更新日期:2008-08-15 00:00:00

  • Tyrosine metabolism in users of oral contraceptives.

    abstract::Brain noradrenaline takes part in the regulation of several brain functions. The formation of brain noradrenaline depends on brain tyrosine (Tyr) levels, which associates with the ratio in plasma of Tyr to other large, neutral amino acids (LNAA). Tyr metabolism has been studied in users of the new generation combined ...

    journal_title:Life sciences

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1016/0024-3205(94)00502-j

    authors: Møller SE,Maach-Møller B,Olesen M,Madsen B,Madsen P,Fjalland B

    更新日期:1995-01-01 00:00:00

  • Vitamin D receptor gene expression in human pituitary gland.

    abstract::1,25-dihydroxyvitamin D3 has important physiological effects such as calcium transport and cell growth and differentiation. These biological effects are mediated by their binding to specific intracellular receptor termed vitamin D receptor (VDR). VDR mRNA expression has been demonstrated in several tissues, but to dat...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(96)00586-3

    authors: Pérez-Fernandez R,Alonso M,Segura C,Muñoz I,García-Caballero T,Diguez C

    更新日期:1997-01-01 00:00:00

  • Effects of cannabinoid receptor ligands on LPS-induced pulmonary inflammation in mice.

    abstract::The effects of cannabinoid receptor agonists WIN 55,212-2, delta9-tetrahydrocannabinol (delta9-THC), arachidonoylethanolamide (anandamide) and palmitoylethanolamide on lipopolysaccharide (LPS) -induced bronchopulmonary inflammation in mice were investigated. WIN 55,212-2 and delta9-THC induced a concentration-dependen...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(98)00324-5

    authors: Berdyshev E,Boichot E,Corbel M,Germain N,Lagente V

    更新日期:1998-01-01 00:00:00

  • Regional brain metabolic activation during craving elicited by recall of previous drug experiences.

    abstract::Cocaine cues elicit craving and physiological responses. The cerebral circuits involved in these are poorly understood. The purpose of this study was to assess the relation between regional brain activation and cocaine cue elicited responses. Thirteen right-handed cocaine abusers were scanned with positron emission to...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(98)00619-5

    authors: Wang GJ,Volkow ND,Fowler JS,Cervany P,Hitzemann RJ,Pappas NR,Wong CT,Felder C

    更新日期:1999-01-01 00:00:00

  • The signal peptide of pro-opiomelancortin: validation of a specific radioimmunoassay.

    abstract::The N-terminus portion of the POMC leader sequence (signal peptide) was synthesized, and an antiserum was raised against it. A radioimmunoassay was developed which is effective at a dilution of 1:500,000, and sensitive at less than 1 fmole/tube. Since leader sequences often exhibit structural homologies, and since syn...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(82)90135-7

    authors: Akil H,Shiomi H,Thompson R,Lax S,Coy D,Watson S

    更新日期:1982-11-15 00:00:00

  • Impact of cardiac-specific expression of CD39 on myocardial infarct size in mice.

    abstract:AIMS:Prior work suggests that ischemic preconditioning increases the level of CD39 in the heart and contributes to cardiac protection. Therefore, we examined if targeted cardiac expression of CD39 protects against myocardial injury. MAIN METHODS:Mice with cardiac-specific expression of human CD39 (αMHC/hCD39-Tg) were ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2016.10.016

    authors: Smith SB,Xu Z,Novitskaya T,Zhang B,Chepurko E,Pu XA,Wheeler DG,Ziolo M,Gumina RJ

    更新日期:2017-06-15 00:00:00

  • High-dose pentazocine antagonizes the antinociception induced by high-dose morphine.

    abstract:AIMS:To investigate the effects of high doses of pentazocine on antinociception induced by a high dose of morphine and the role of the kappa-opioid receptors (KORs) in these effects in mice. MAIN METHODS:Sixty-six C57BL/6J mice were pretreated with a KOR antagonist, nor-binaltorphimine (nor-BNI) (10mg·kg(-1)), or a no...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2015.02.023

    authors: Shu H,Wang Z,Ye F,Li Q,Dou Y,Lin Y,Huang W,Xiao X

    更新日期:2015-06-01 00:00:00

  • Decreased Na,K-ATPase gene expression in cardiomyopathic hamster hearts.

    abstract::We studied Na,K-ATPase mRNA expression in cardiomyopathic (Bio 14.6) and normal (F1b) Syrian hamster ventricles. In Northern blot analysis, Na,K-ATPase alpha 1, alpha 2, alpha 3 and beta 1 isoform mRNAs were detected in 3-week-old Bio 14.6 and F1b hamster ventricles. We then investigated the expression of alpha 1 subu...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(94)00776-4

    authors: Tsuruya Y,Ikeda U,Yamamoto K,Seino Y,Kanbe T,Shimada K

    更新日期:1994-01-01 00:00:00

  • Synthetic human adrenomedullin and ADM15-52 have potent short-lasting vasodilator activity in the pulmonary vascular bed of the cat.

    abstract::Responses to synthetic human adrenomedullin, a novel hypotensive peptide localized in several organ systems, including the lung, and the carboxy terminal 15-52 amino acid fragment of adrenomedullin (ADM15-52) were investigated in the pulmonary vascular bed of the intact-chest cat. Under constant flow conditions when b...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(94)00246-0

    authors: Cheng DY,DeWitt BJ,Wegmann MJ,Coy DH,Bitar K,Murphy WA,Kadowitz PJ

    更新日期:1994-01-01 00:00:00