KF17837: a novel selective adenosine A2A receptor antagonist with anticataleptic activity.

Abstract:

:KF17837 is a novel selective adenosine A2A receptor antagonist. Oral administration of KF17837 (2.5, 10.0 and 30.0 mg/kg) significantly ameliorated the cataleptic responses induced by intracerebroventricular administration of an adenosine A2A receptor agonist, CGS 21680 (10 micrograms), in a dose-dependent manner. KF17837 also reduced the catalepsy induced by haloperidol (1 mg/kg i.p.) and by reserpine (5 mg/kg i.p.). These anticataleptic effects were exhibited dose dependently at doses from 0.625 and 2.5 mg/kg p.o., respectively. Moreover, KF17837 (0.625 mg/kg p.o.) potentiated the anticataleptic effects of a subthreshold dose of L-3,4-dihydroxyphenylalanine (L-DOPA; 25 mg/kg i.p.) plus benserazide (6.25 mg/kg i.p.). These results suggested that KF17837 is a centrally active adenosine A2A receptor antagonist and that the dopaminergic function of the nigrostriatal pathway is potentiated by adenosine A2A receptor antagonists. Furthermore, KF17837 may be a useful drug in the treatment of parkinsonism.

journal_name

Eur J Pharmacol

authors

Kanda T,Shiozaki S,Shimada J,Suzuki F,Nakamura J

doi

10.1016/0014-2999(94)90551-7

subject

Has Abstract

pub_date

1994-05-02 00:00:00

pages

263-8

issue

3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(94)90551-7

journal_volume

256

pub_type

杂志文章
  • Evaluation of deprenyl for cocaine-like discriminative stimulus effects in rats.

    abstract::The antiparkinsonian agent l-deprenyl is metabolized to l-methamphetamine and l-amphetamine and, at higher doses, can facilitate the release and inhibit the reuptake of dopamine. Since l-deprenyl can affect dopamine release and reuptake it was important to evaluate it for cocaine-like discriminative stimulus effects. ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90650-5

    authors: Yasar S,Schindler CW,Thorndike EB,Goldberg SR

    更新日期:1994-07-11 00:00:00

  • Peroxisome proliferator-activated receptor gamma agonists as therapy for chronic airway inflammation.

    abstract::Peroxisome proliferator-activated receptor gamma (PPARgamma) is a ligand-activated transcription factor belonging to the nuclear hormone receptor superfamily. PPARgamma regulates several metabolic pathways by binding to sequence-specific PPAR response elements in the promoter region of target genes, including lipid bi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2005.12.048

    authors: Belvisi MG,Hele DJ,Birrell MA

    更新日期:2006-03-08 00:00:00

  • Influence of the periprostatic adipose tissue in obesity-associated mouse urethral dysfunction and oxidative stress: Effect of resveratrol treatment.

    abstract::Obese mice display overactive bladder (OAB) associated with impaired urethra smooth muscle (USM) function. In this study, we evaluated the role of the adipose tissue surrounding the urethra and prostate in obese mice (here referred as periprostatic adipose tissue; PPAT) to the USM dysfunction. Male C57BL6/JUnib mice f...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.08.010

    authors: Alexandre EC,Calmasini FB,Sponton ACDS,de Oliveira MG,André DM,Silva FH,Delbin MA,Mónica FZ,Antunes E

    更新日期:2018-10-05 00:00:00

  • Linoleic and dihomo-gamma-linolenic acids modulate granuloma growth and granuloma macrophage eicosanoid release.

    abstract::We have already demonstrated that arachidonic acid (AA) inhibits carrageenin-induced granuloma growth in vivo and that this effect is related to an increase in prostaglandin E2 formation. As prostaglandin E1 has been shown to be more effective in inhibiting granuloma growth than prostaglandin E2 we investigated the ef...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90234-7

    authors: Elliott GR,Adolfs MJ,Van Batenburg M,Bonta IL

    更新日期:1986-05-27 00:00:00

  • Potentiation by alcuronium of the antimuscarinic effect of N-methylscopolamine in guinea pig left atria.

    abstract::Alcuronium is known to stabilize allosterically the binding of the muscarinic antagonist N-methylscopolamine to muscarinic M2 receptors and thus to elevate the equilibrium binding of N-methylscopolamine in homogenized cardiac tissue. In order to check for a functional consequence of this effect, the action of alcuroni...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)00664-s

    authors: Maass A,Kostenis E,Mohr K

    更新日期:1995-01-05 00:00:00

  • Localization of beta 2-adrenoceptor messenger RNA in human and rat lung using in situ hybridization: correlation with receptor autoradiography.

    abstract::We have used in situ hybridization to study the localization of mRNA encoding the beta 2-adrenoceptor in tissue sections of the human and rat lung and compared this with the distribution of beta 2-receptor binding sites using receptor autoradiography. To localize beta 2-receptor mRNA, a [32P]labeled antisense RNA prob...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(91)90021-9

    authors: Hamid QA,Mak JC,Sheppard MN,Corrin B,Venter JC,Barnes PJ

    更新日期:1991-02-25 00:00:00

  • Reduction of myocardial infarct size by SM-20550, a novel Na(+)/H(+) exchange inhibitor, in rabbits.

    abstract::The effects of N-(aminoiminomethyl)-1, 4-dimethyl-1H-indole-2-carboxamide methanesulfonic acid (SM-20550), a novel potent Na(+)/H(+) exchanger, and nicorandil, a K(+) channel opener with nitrate-like activity, were studied in a myocardial ischemia and reperfusion injury model. Anesthetized rabbits underwent occlusion ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00610-5

    authors: Yamada K,Matsui K,Satoh K,Kitano M,Yamamoto S,Ohashi N

    更新日期:2000-09-15 00:00:00

  • Differential effects of selective and non-selective inhibition of nitric oxide synthase on the expression and activity of cyclooxygenase-2 during gastric ulcer healing.

    abstract::Nitric oxide synthases (NOS) and cyclooxygenase-2 (COX-2) are important enzymes involved in ulcer healing but interactions between them have not been clearly defined. The aim of this study was to investigate the effects of selective or non-selective inhibition of NOS on the expression and activity of COX-2 during heal...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.12.088

    authors: Guo JS,Cho CH,Wang JY,Koo MW

    更新日期:2006-05-01 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

  • Effects of deficiency of the G protein Gsα on energy and glucose homeostasis.

    abstract::G(s)α is a ubiquitously expressed G protein α-subunit that couples receptors to the generation of intracellular cyclic AMP. The G(s)α gene GNAS is a complex gene that undergoes genomic imprinting, an epigenetic phenomenon that leads to differential expression from the two parental alleles. G(s)α is imprinted in a tiss...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2010.10.105

    authors: Chen M,Nemechek NM,Mema E,Wang J,Weinstein LS

    更新日期:2011-06-11 00:00:00

  • Inhibition by tamsulosin of tension responses of human hyperplastic prostate to electrical field stimulation.

    abstract::Tamsulosin (10(-10)-10(-9) M) or prazosin (10(-9)-10(-8) M) concentration dependently blocked the tension responses to electrical field stimulation (0.3 ms duration, 80 V and 20 Hz) in human hyperplastic prostate with lC50 values of (1.93 +/- 0.26) x 10(-10) M and (2.11 +/- 0.21) x 10(-9) M, respectively. The relative...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(96)00197-5

    authors: Chueh SC,Guh JH,Chen J,Lai MK,Ko FN,Teng CM

    更新日期:1996-06-03 00:00:00

  • Chronic mianserin treatment decreases 5-HT2 receptor binding without altering 5-HT2 receptor mRNA levels.

    abstract::Rats were injected with 15 mg/kg (i.p.) mianserin or vehicle (saline) for 4, 10 or 21 days and 5-HT2 receptor binding and mRNA levels measured. Treatment with mianserin induced a substantial decrease in 5-HT2 radioligand binding (44-59% decrease; P less than 0.05 vs. control). No changes in the amount of 5-HT2 or, as ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(91)90093-w

    authors: Roth BL,Ciaranello RD

    更新日期:1991-06-19 00:00:00

  • Tissue selectivity of substance P alkyl esters: suggesting multiple receptors.

    abstract::Previous studies from this laboratory suggested that two subtypes of substance P receptor may exist, based on the observations that substance P and related peptides did not exhibit complete cross-desensitisation on guinea-pig ileum, and that two distinct rank orders of potency of tachykinins were observed in various t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90052-3

    authors: Watson SP,Sandberg BE,Hanley MR,Iversen LL

    更新日期:1983-01-28 00:00:00

  • CS-045, a new oral antidiabetic agent, stimulates fructose-2,6-bisphosphate production in rat hepatocytes.

    abstract::Fructose-2,6-bisphosphate is a potent activator of 6-phosphofructo-1-kinase, a key enzyme in glycolysis. We previously revealed that sulfonylureas stimulate fructose-2,6-bisphosphate production in the rat liver by activating 6-phosphofructo-2-kinase. In the present study, we show that CS-045, a new antidiabetic agent,...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90462-6

    authors: Murano K,Inoue Y,Emoto M,Kaku K,Kaneko T

    更新日期:1994-03-21 00:00:00

  • Intracerebroventricular morphine produces diuresis 24 h after previous dynorphin/morphine treatment.

    abstract::The effect of dynorphin A-(1-13) on morphine-induced urine output was studied in the rat. The previous simultaneous intracerebroventricular (i.c.v.) injection of dynorphin (20 micrograms/rat) and morphine (20 micrograms/rat) altered the response of rat given morphine (20 micrograms/rat) 24 h later, producing a 3-fold ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90015-4

    authors: Hong O,Young GA,Khazan N

    更新日期:1986-12-02 00:00:00

  • Anticancer effects and possible mechanisms of lycopene intervention on N-methylbenzylnitrosamine induced esophageal cancer in F344 rats based on PPARγ1.

    abstract::Lycopene, a natural carotenoid, has potential chemopreventive effects in many cancers. This study aimed to examine the effects of lycopene on regulating the inflammation and apoptosis of N-nitrosomethylbenzylamine(NMBzA) induced esophageal cancer in F344 rats. After the rats were fed normal diets containing different ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173230

    authors: Cui L,Xu F,Wu K,Li L,Qiao T,Li Z,Chen T,Sun C

    更新日期:2020-08-15 00:00:00

  • Exploration of Emodin to treat alpha-naphthylisothiocyanate-induced cholestatic hepatitis via anti-inflammatory pathway.

    abstract::Emodin, 1,3,8-trihydroxy-6-methyl-anthraquinone, is an anthraquinone derivative from the roots of Rheum officinale Baill that has been used to treat many diseases in digestive system for thousands of years. This study is to disclose the mechanism of Emodin to treat cholestatic hepatitis via anti-inflammatory pathway. ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.06.044

    authors: Ding Y,Zhao L,Mei H,Zhang SL,Huang ZH,Duan YY,Ye P

    更新日期:2008-08-20 00:00:00

  • Prostacyclin mediates the potentiated hypotensive effect of bradykinin following captopril treatment.

    abstract::The effect of angiotensin-converting enzyme inhibition by captopril on the release of a prostacyclin-like substance by bradykinin, angiotensin I and angiotensin II was studied by means of the blood-bathed bioassay technique of Vane. Administration of captopril abolished the release of prostacyclin-like substance induc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(80)90468-9

    authors: Mullane KM,Moncada S

    更新日期:1980-09-05 00:00:00

  • The effect of metformin on carotid intima-media thickness (CIMT): A systematic review and meta-analysis of randomized clinical trials.

    abstract::Metformin administration has been reported to influence the carotid intima-media thickness (CIMT) in humans. However, since previously conducted studies have yielded inconsistent results, the exact effect of metformin on CIMT remains unclear. Causes that could lead to inconsistency in reported research could be the du...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173458

    authors: Chen Y,Li H,Ye Z,Găman MA,Tan SC,Zhu F

    更新日期:2020-11-05 00:00:00

  • Histamine release induced by neurotensin from rat peritoneal mast cells.

    abstract::Neurotensin induced the release of histamine from both purified and non-purified rat peritoneal mast cells by a non-cytotoxic mechanism. It was effective at a concentration as low as 10(-8) M. The dose-response curve for the neurotensin effect was triphasic: and initial gentle rise, a plateau (2.5 X 10(-7) -2.5 X 10(-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(81)90494-5

    authors: Kurose M,Saeki K

    更新日期:1981-12-03 00:00:00

  • [D-Met2,Pro5]enkephalinamide activates cardioinhibitory efferents in anaesthetized dogs.

    abstract::[D-Met2,Pro5]enkephalinamide (DMPEA) strongly activated cardioinhibitory vagal efferents and elicited bradycardia when perfused through the cerebroventricular system of anaesthetized dogs. These effects were concentration-dependent but plateaued at an intraventricular concentration of 200 micrograms/ml. At this maxima...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90216-x

    authors: Inoue K,Nashan B,Arndt JO

    更新日期:1985-04-02 00:00:00

  • Effects of yohimbine on naloxone-induced antinociception in a rat model of inflammatory hyperalgesia.

    abstract::Effects of the alpha2-adrenoceptor antagonist yohimbine on the antinociception produced by a low dose of naloxone were examined in a rat model of carrageenan-induced inflammation. In rats receiving saline prior to naloxone injection, the low dose of naloxone (5 microg/kg, i.p.) significantly prolonged paw withdrawal l...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00151-4

    authors: Tsuruoka M,Hiruma Y,Matsutani K,Matsui Y

    更新日期:1998-05-08 00:00:00

  • Involvement of the melanocortin MC4 receptor in stress-related behavior in rodents.

    abstract::The melanocortin subtype 4 (MC4) receptor has been postulated to be involved in stress and stress-related behavior. We made use of melanocortin MC4 receptor agonists and antagonist to investigate the relationship between the melanocortin MC4 receptor and stress related disorders. The nonspecific melanocortin receptor ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)02033-8

    authors: Chaki S,Ogawa S,Toda Y,Funakoshi T,Okuyama S

    更新日期:2003-08-01 00:00:00

  • Factor Xa inhibitors differently modulate electrical activities in pulmonary veins and the sinoatrial node.

    abstract::Factor Xa inhibitors reduce stroke in patients with atrial fibrillation. Pulmonary veins (PVs) and the sinoatrial node (SAN) are crucial for genesis of atrial fibrillation. However, the electrophysiological effects of factor Xa inhibitors (edoxaban and rivaroxaban) on PVs and the SAN remain unclear. Conventional micro...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.07.003

    authors: Chang CJ,Cheng CC,Chen YC,Higa S,Huang JH,Chen SA,Chen YJ

    更新日期:2018-08-15 00:00:00

  • Pannexin-1 channels do not regulate α1-adrenoceptor-mediated vasoconstriction in resistance arteries.

    abstract::Recent reports have provided evidence for a new concept that in small resistance arteries α1D-adrenoceptor-mediated contraction is intimately linked to pannexin-1 (Px1) hemichannels that open to allow the release of ATP, from the smooth muscle effector cell, that acts back on P2Y purinoceptors to cause contraction. Th...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2015.01.024

    authors: Angus JA,Betrie AH,Wright CE

    更新日期:2015-03-05 00:00:00

  • Reversal of scopolamine-induced deficits in radial maze performance by (-)-huperzine A: comparison with E2020 and tacrine.

    abstract::The effects of (-)-huperzine A ((5R,9R,11E)-5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-5, 9-methanocycloocta[b]pyridin-2(1H)-one), and of the hydrochloride salt of E2020 ((R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]-methyl piperidine) and tacrine (9-amino-1,2,3,4-tetrahydroacridine), on the scopolamine-in...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00199-x

    authors: Wang T,Tang XC

    更新日期:1998-05-22 00:00:00

  • Antifibrillatory actions of bepridil and butyl-MDI, two intracellular calcium antagonists.

    abstract::The antifibrillatory and electrophysiologic actions of bepridil and butyl-methylenedioxyindene (BU-MDI), two intracellular calcium antagonists, were examined in anesthetized dogs. The administration of bepridil (1.0-10.0 mg/kg i.v.) significantly increased the electrical threshold for ventricular fibrillation determin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90107-4

    authors: Lynch JJ,Rahwan RG,Lucchesi BR

    更新日期:1985-04-23 00:00:00

  • Influence of pharmacologically-induced experimental anxiety on nociception and antinociception in rats.

    abstract::Animal studies reveal that diverse environmental stimuli that generate anxiety-like behaviors also induce antinociception; conversely, clinical data show that pain perception is reduced under anxiolysis. This study was conducted to investigate the influence of pharmacologically induced-anxiety on nociception and antin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.06.060

    authors: Jiménez-Velázquez G,Fernández-Guasti A,López-Muñoz FJ

    更新日期:2006-10-10 00:00:00

  • ABT-866, a novel alpha(1A)-adrenoceptor agonist with antagonist properties at the alpha(1B)- and alpha(1D)-adrenoceptor subtypes.

    abstract::N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide, maleate (ABT-866) is a novel alpha(1)-adrenoceptor agent with mixed pharmacological properties in vitro. Compared to phenylephrine, ABT-866 demonstrates intrinsic activity at the alpha(1A)-adrenoceptor subtype present in the rabbit urethra (pD(2) = 6.22, with 80% ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)01976-3

    authors: Buckner SA,Milicic I,Daza AV,Meyer MD,Altenbach RJ,Williams M,Sullivan JP,Brioni JD

    更新日期:2002-08-02 00:00:00

  • Resveratrol modifies risk factors for coronary artery disease in swine with metabolic syndrome and myocardial ischemia.

    abstract::Resveratrol has been purported to modify risk factors for obesity and cardiovascular disease. We sought to examine the effects of resveratrol in a porcine model of metabolic syndrome and chronic myocardial ischemia. Yorkshire swine were fed either a normal diet (control), a high cholesterol diet (HCD), or a high chole...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.04.059

    authors: Robich MP,Osipov RM,Chu LM,Han Y,Feng J,Nezafat R,Clements RT,Manning WJ,Sellke FW

    更新日期:2011-08-16 00:00:00