A novel methylthio metabolite of s-triazolo[3,4-a]phthalazine, a lead compound for the development of antianxiety drugs, in rats.

Abstract:

:When s-triazolo[3,4-a]phthalazine (Tri-P) was orally administered in rats, a more lipophilic metabolite M-1 than the parent compound was isolated from the urine. The metabolite M-1 was identified as 7-methylthio Tri-P by means of high resolution MS and two-dimensional NMR spectrometry. Furthermore, the 7-methylthio conjugate was generated from the parent compound Tri-P in isolated rat hepatocytes. Although the contribution of the intestinal microflora to the formation of methylthio metabolite has been pointed out so far, the limited data in this study lead us to conclude that the liver plays a role in all metabolic reactions of Tri-P to its 7-methylthio conjugate in rats.

journal_name

Life Sci

journal_title

Life sciences

authors

Imamura Y,Noda A,Imamura T,Ono Y,Okawara T,Noda H

doi

10.1016/j.lfs.2003.06.032

subject

Has Abstract

pub_date

2003-11-21 00:00:00

pages

29-36

issue

1

eissn

0024-3205

issn

1879-0631

pii

S0024320503009068

journal_volume

74

pub_type

杂志文章
  • Alpha-melanocyte stimulating hormone (MSH) antagonizes the anorexia by corticotropin releasing factor (CRF).

    abstract::We examined a hypothesis that alpha-Melanocyte Stimulating Hormone (MSH) can antagonizes the anorexia induced by intracerebroventricular injection of corticotropin releasing factor (CRF). Food intake of the rats deprived of food for 18 h was significantly inhibited by 4 h after intracerebroventricular injection of CRF...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(93)90620-i

    authors: Oohara M,Negishi M,Shimizu H,Sato N,Mori M

    更新日期:1993-01-01 00:00:00

  • Hyperpolarization contributes to vascular hyporeactivity in rats with lipopolysaccharide-induced endotoxic shock.

    abstract::We have examined the role of membrane hyperpolarization in mediating vascular hyporeactivity induced by bacterial lipopolysaccharide (LPS) in endothelial-denuded strips of rat thoracic aorta ex vivo. The injection of rats with LPS caused a significant fall of blood pressure and a severe vascular hyporeactivity to nore...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(00)00978-4

    authors: Chen SJ,Wu CC,Yang SN,Lin CI,Yen MH

    更新日期:2000-12-29 00:00:00

  • Endothelin-1 plasma levels and vascular endothelial dysfunction in primary open angle glaucoma.

    abstract:AIMS:To assess the relationship between endothelial dysfunction, endothelin 1 (ET-1) plasma levels and subclinical inflammation in primary open angle glaucoma (POAG) patients. MAIN METHODS:We enrolled 40 POAG patients with progressive visual field damage, although well controlled intraocular pressure (IOP) and compare...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2012.02.013

    authors: Cellini M,Strobbe E,Gizzi C,Balducci N,Toschi PG,Campos EC

    更新日期:2012-10-15 00:00:00

  • Effects of morphine on the phenotypic expression of cell surface markers on murine lymphocytes.

    abstract::There is a growing literature indicating that opioid abuse by human addicts and opioid administration to animals have profound effects on the immune system. In the present study, implantation of morphine pellets in mice was associated with reduced phenotypic expression of the cell surface antigens specific to T-lympho...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(92)90607-q

    authors: Kimes AS,Smith WJ,Winchell CJ,London ED

    更新日期:1992-01-01 00:00:00

  • Unique modulation of central 5-HT2 receptor binding sites and 5-HT2 receptor-mediated behavior by continuous gepirone treatment.

    abstract::The effect of continuous treatment with the selective 5-HT1A agonist gepirone upon 5-HT2-mediated behavior and cortical 5-HT2 receptor binding sites was examined in naive rats or rats receiving noradrenergic (DSP4) or serotonergic (5,7-DHT) lesions. Continuous administration of gepirone in non-lesioned rats for 3, 7, ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(91)90478-t

    authors: Yocca FD,Eison AS,Hyslop DK,Ryan E,Taylor DP,Gianutsos G

    更新日期:1991-01-01 00:00:00

  • Cocaine-induced changes in 3H-naloxone binding in brain membranes isolated from spontaneously hypertensive and Wistar-Kyoto rats.

    abstract::Effects of sub-acute cocaine treatment on 3H-naloxone binding to 6 brain regions were examined in spontaneously hypertensive (SHR) and Wistar-Kyoto (WKY) rats. Cocaine hydrochloride (3 mg/kg, i.v.) was given by bolus injection daily for five days. Rats were decapitated 24 hr following the final injection and crude mem...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(88)90421-3

    authors: Ishizuka Y,Rockhold RW,Hoskins B,Ho IK

    更新日期:1988-01-01 00:00:00

  • Sodium nitroprusside activates p38 mitogen activated protein kinase through a cGMP/PKG independent mechanism.

    abstract::The objective of this study was to understand the mechanism of action of nitric oxide (NO) in the heart by determining whether nitric oxide (NO) released from sodium nitroprusside (SNP) induces p38 mitogen activated protein kinase (p38 MAPK) phosphorylation and whether this is mediated through a cyclic GMP (cGMP)/prot...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2007.06.022

    authors: Rabkin SW,Klassen SS,Tsang MY

    更新日期:2007-08-02 00:00:00

  • The effect of chromium on rat insulinoma cells in high glucose conditions.

    abstract:AIMS:it has been suggested that Chromium (Cr), one of the essential minerals, can be beneficial to type 2 diabetic patients because it lowers blood glucose levels by improving various steps in insulin action. A few studies reported that Cr might also have some beneficial effects in people with type 1 diabetes mellitus ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2010.08.001

    authors: Kwon MJ,Chung HS,Yoon CS,Ko JH,Jun HJ,Kim TK,Lee SH,Ko KS,Rhee BD,Kim MK,Park JH

    更新日期:2010-09-25 00:00:00

  • Augmented analgesic effects of L-tryptophan combined with low current transcranial electrostimulation.

    abstract::The analgesic effects of low current transcranial electrostimulation are both naloxone and pCPA-reversible, suggesting that they may be mediated in part by endogenous opioid and serotonergic activity. The present experiments indicate that pretreatment with the serotonin precursor L-tryptophan results in an increased a...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(90)90583-d

    authors: Malin DH,Lake JR,Hamilton RF,Skolnick MH

    更新日期:1990-01-01 00:00:00

  • Involvement of K+ channels and calcium-dependent pathways in the action of T3 on amino acid accumulation and membrane potential in Sertoli cells of immature rat testis.

    abstract::The purpose of this study was to investigate the involvement of calcium in K+ currents and its effects on amino acid accumulation and on the membrane potential regulated by tri-iodo-L-thyronine (T3) in Sertoli cells. Immature rat testes were pre-incubated for 30 min in Krebs-Ringer bicarbonate buffer and incubated for...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2003.08.005

    authors: Volpato KC,Menegaz D,Leite LD,Barreto KP,de Vilhena Garcia E,Silva FR

    更新日期:2004-01-23 00:00:00

  • Effects of FR145237, an acyl-CoA:cholesterol acyltransferase inhibitor, on diet-induced hypercholesterolemia in diabetic rats.

    abstract::Recent studies have shown that acyl-CoA:cholesterol acyltransferase (ACAT) plays an important role in the initiation of diabetes-associated hypercholesterolemia. To confirm this hypothesis, effects of a potent ACAT inhibitor, FR145237, on diet-induced hypercholesterolemia were examined in streptozotocin (STZ)-induced ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(96)00658-3

    authors: Sakuma Y,Hagihara H,Nagayoshi A,Ohne K,Mutoh S,Ito Y,Nakahara K,Notsu Y,Okuhara M

    更新日期:1997-01-01 00:00:00

  • The influence of alpha-fluoromethylhistidine and histamine receptor antagonists on the beta-endorphin-induced corticosterone response.

    abstract::Involvement of a central histaminergic mechanism in the stimulating effect of beta-endorphin (beta-End) on the pituitary-adrenocortical activity, measured indirectly through corticosterone secretion, was investigated in conscious rats. The rise in serum corticosterone levels, induced by beta-End injected intraventricu...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(91)90458-n

    authors: Turoń M,Tytoń J,Bugajski J

    更新日期:1991-01-01 00:00:00

  • The antidepressant mechanism of Hypericum perforatum.

    abstract::Clinical data indicate that hydroalcoholic extracts of Hypericum perforatum might be as valuable as conventional antidepressants in mild-to-moderate depression, with fewer side effects. One clinical trial using two extracts with different hyperforin contents indicated it as the main active principle responsible for th...

    journal_title:Life sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.lfs.2004.04.005

    authors: Mennini T,Gobbi M

    更新日期:2004-07-16 00:00:00

  • Selective G2/M arrest in a p53(Val135)-transformed cell line induced by lithium is mediated through an intricate network of MAPK and β-catenin signaling pathways.

    abstract:AIMS:Lithium is a common mood stabilizer to treat bipolar disorder. It has a narrow window of therapeutic action and its mechanism of action and possible side effects are still not fully understood. Lithium is a potent inhibitor of glycogen synthase kinase 3β (GSK-3β). Previous studies indicated that lithium can induce...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2012.07.027

    authors: Tsui MM,Tai WC,Wong WY,Hsiao WL

    更新日期:2012-09-24 00:00:00

  • Nanoparticles designed to regulate tumor microenvironment for cancer therapy.

    abstract::Increasing understanding in tumor pathology reveals that tumor microenvironment (TME), which supports tumor progression and poses barriers for available therapies, takes a great responsibility in inefficient treatment and poor prognosis. In recent years, the versatile nanotechnology employed in TME regulation has made...

    journal_title:Life sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.lfs.2018.03.044

    authors: Li M,Zhang F,Su Y,Zhou J,Wang W

    更新日期:2018-05-15 00:00:00

  • A potent nonpeptide neuropeptide Y Y1 receptor antagonist, a benzodiazepine derivative.

    abstract::We describe here a nonpeptide neuropeptide Y Y1 receptor antagonist, 2,4-dioxo-1,5-bis(2-oxo-2-orthotolyl-ethyl)-3-[3-[3-([3-[3-(3-p iperidin-1-ylmethyl-phenoxy)-propylcarbamoyl]-propyl]-car bamoyloxymethyl)-phenyl]-ureido]-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diaz epine (Compound 1), which was previously synthesized as...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(98)00357-9

    authors: Shigeri Y,Ishikawa M,Ishihara Y,Fujimoto M

    更新日期:1998-01-01 00:00:00

  • A guinea pig ileum preparation devoid of functional kappa receptors: a new in vitro pharmacologic assay for mu-opioid ligands.

    abstract::Guinea pig ileum longitudinal muscle/myenteric plexus preparations contain functional mu- and kappa-opioid receptors. A preparation with blocked kappa receptors was obtained by pretreating guinea pigs with 0.1-10.0 mg/kg intraperitoneal doses of a new kappa-selective affinity label, DIPPA (2-(3,4-dichlorophenyl)-N-met...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(97)00076-3

    authors: Schwartz RW,Chang AC,Portoghese PS,Berzetei-Gurske IP

    更新日期:1997-01-01 00:00:00

  • Effect of fudosteine, a cysteine derivative, on airway hyperresponsiveness, inflammation, and remodeling in a murine model of asthma.

    abstract:AIMS:Fudosteine is a cysteine derivative that is used as an expectorant in chronic bronchial inflammatory disorders. It has been shown to decrease the number of goblet cells in an animal model. This study examined the effects of fudosteine on airway inflammation and remodeling in a murine model of chronic asthma. MAIN...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2013.03.022

    authors: Ueno-Iio T,Shibakura M,Iio K,Tanimoto Y,Kanehiro A,Tanimoto M,Kataoka M

    更新日期:2013-05-30 00:00:00

  • Thromboxane A2 synthetase inhibition suppresses cough induced by angiotensin converting enzyme inhibitors.

    abstract::Based on our earlier animal study, we became interested to investigate if thromboxane A2 (TXA2) is involved in angiotensin converting enzyme (ACE) induced cough in man. To 11 patients with hypertension, who had developed cough induced by ACE inhibitors, a TXA2 synthetase inhibitor, ozagrel was given for 1 to 2 months ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(97)00124-0

    authors: Umemura K,Nakashima M,Saruta T

    更新日期:1997-01-01 00:00:00

  • Proteomic analysis of honokiol-induced cytotoxicity in thyroid cancer cells.

    abstract:AIMS:Honokiol is a natural product extracted from herbal plants such as the Magnolia species which have been shown to exhibit anti-tumor and anti-metastatic properties. However, the effects of honokiol on thyroid cancers are largely unknown. MATERIALS AND METHODS:To determine whether honokiol might be useful for the t...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2018.06.002

    authors: Chou HC,Lu CH,Su YC,Lin LH,Yu HI,Chuang HH,Tsai YT,Liao EC,Wei YS,Yang YT,Chien YA,Yu XR,Lee YR,Chan HL

    更新日期:2018-08-15 00:00:00

  • Functional studies with the opioid peptide dynorphin: acute effects of injections into the substantia nigra reticulata of naive rats.

    abstract::When injected into the substantia nigra reticulata of naive rats, dynorphin-(1-17) caused a dose dependent contralateral rotation which was inhibited by naloxone in a dose dependent manner. Met-enkephalin injected in the same coordinates as the ones used with dynorphin also induced rotation but of lower intensity, whi...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(83)90563-5

    authors: Herrera-Marschitz M,Hökfelt T,Ungerstedt U,Terenius L

    更新日期:1983-01-01 00:00:00

  • 4-Aminopyridine antagonizes the acute relaxant action of metformin on adrenergic contraction in the ventral tail artery of the rat.

    abstract::The ability of metformin (MF) to acutely relax phenylephrine (PE)-induced contraction in the isolated rat tail artery is reported to be accompanied by repolarization of the arterial smooth muscle cell (SMC) membranes. These membranes contain potassium (K) channels which if opened could mediate such repolarization and ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(99)00522-6

    authors: Peuler JD,Lee JM,Smith JM

    更新日期:1999-10-29 00:00:00

  • Antagonistic effect of urea on oxygenation-linked binding of ATP in an elasmobranch hemoglobin.

    abstract::The O2 affinity of "stripped" (cofactor-free) hemoglobin (Hb) of the elasmobranch, Squalus acanthias is decreased by ATP, the main erythrocytic phosphate cofactor but increased by urea at physiological concentration. When both compounds are present, as in life, urea decreases the ATP sensitivity, indicating that previ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(83)90105-4

    authors: Weber RE,Wells RM,Tougaard S

    更新日期:1983-05-02 00:00:00

  • Changes in renal, platelet and cardiac nitrobenzylthioinosine binding in spontaneously hypertensive rats.

    abstract::In an attempt to investigate the role of nucleoside transporter function in the hypertensive state, we have compared the binding of [3H]nitrobenzylthioinosine ([3H]NBMPR), a nucleoside transporter probe, in membranes prepared from platelet, renal, pulmonary, cardiac and brain tissues of spontaneously hypertensive rats...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(90)90024-l

    authors: Williams EF,Udofia UP,Brooks GR,Hawk NN

    更新日期:1990-01-01 00:00:00

  • Polynitroxyl albumin plus tempol attenuates liver injury and inflammation after hepatic ischemia and reperfusion.

    abstract::PNA+Tempol, albumin containing conjugated (polynitroxyl albumin; PNA) and free (4-hydroxyl-2,2,6,6-tetramethyl-piperidinyl-1-oxyl; Tempol) nitroxide may protect against injury caused by reactive oxygen species. Therefore, the actions of PNA+Tempol on liver injury and inflammation induced by hepatic ischemia and reperf...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(00)00907-3

    authors: Blonder JM,McCalden TA,Hsia CJ,Billings RE

    更新日期:2000-11-17 00:00:00

  • Autophagy alleviates mitochondrial DAMP-induced acute lung injury by inhibiting NLRP3 inflammasome.

    abstract:AIM:Acute lung injury (ALI) is characterized by alveolar macrophage overactivation and uncontrolled pulmonary inflammation. Mitochondrial damage-associated molecular patterns (MTDs), one type of damage-associated molecular patterns (DAMPs) released from ruptured mitochondrial, can induce inflammation which participates...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2020.118833

    authors: Peng W,Peng F,Lou Y,Li Y,Zhao N,Shao Q,Chen J,Qian K,Zeng Z,Zhan Y,Jiang R,Liu F

    更新日期:2021-01-15 00:00:00

  • Leukotriene D4 role in allergic asthma pathogenesis from cellular and therapeutic perspectives.

    abstract::Asthma is a chronic inflammatory and allergic disease that is mainly characterized by reversible airway obstruction and bronchial hyperresponsiveness. The incidence of asthma is increasing with more than 350 million people worldwide are affected. Up to now, there is no therapeutic option for asthma and most of the pre...

    journal_title:Life sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.lfs.2020.118452

    authors: Al-Azzam N,Elsalem L

    更新日期:2020-11-01 00:00:00

  • Structural and histomorphometric evaluations of ferutinin effects on the uterus of ovariectomized rats during osteoporosis treatment.

    abstract:AIMS:The effects of chronic administration of Ferutinin (phytoestrogen found in the plants of genus Ferula), compared with those elicited by estradiol benzoate, were evaluated, following ovariectomy, on the uterus of ovariectomized rats as regard weight, size, structure and histomorphometry. MAIN METHODS:The experimen...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2011.11.001

    authors: Ferretti M,Bertoni L,Cavani F,Benincasa M,Sena P,Carnevale G,Zavatti M,Viesti VD,Zanoli P,Palumbo C

    更新日期:2012-01-16 00:00:00

  • Extracellular superoxide dismutase ameliorates streptozotocin-induced rat diabetic nephropathy via inhibiting the ROS/ERK1/2 signaling.

    abstract:AIM:Diabetic nephropathy is the leading cause of end stage renal disease in developed countries throughout the world. The imbalance between the production of reactive oxygen species (ROS) and the antioxidant defense system is the main problem that is responsible for the progression of diabetic kidney disease. In this s...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2015.04.018

    authors: Kuo CW,Shen CJ,Tung YT,Chen HL,Chen YH,Chang WH,Cheng KC,Yang SH,Chen CM

    更新日期:2015-08-15 00:00:00

  • New insights into the gene expression associated to amyotrophic lateral sclerosis.

    abstract::Amyotrophic lateral sclerosis (ALS) is the most prevalent neuromuscular disease worldwide. It is a lethal and progressive neurodegenerative disease, principally affecting motor neurons; patient clinical characteristics are muscle weakness, dysphagia and respiratory failure. The mean age is related to family history (4...

    journal_title:Life sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.lfs.2017.12.016

    authors: Recabarren-Leiva D,Alarcón M

    更新日期:2018-01-15 00:00:00