Comparison of short-term administration of sertindole, clozapine and haloperidol on the inactivation of midbrain dopamine neurons in the rat.

Abstract:

:The present study describes the effect of sertindole, clozapine and haloperidol on the number of spontaneously active dopamine neurons in ventral tegmental area and substantia nigra pars compacta after daily oral treatment for 1, 2 or 3 weeks. In general, daily administration of high dosages (sertindole: 2.8 mumol/kg/day, clozapine: 60 mumol/kg/day, haloperidol: 0.43 mumol/kg/day) induced no statistically significant decrease in the number of active dopamine neurons within the first 2 weeks of treatment. All three compounds induced a marked effect in ventral tegmental area after administration for 3 weeks, but only sertindole and haloperidol influenced the activity in substantia nigra pars compacta. This result is in accordance with clinical data where the antipsychotic effect is observed after 2-3 weeks of treatment.

journal_name

Eur J Pharmacol

authors

Skarsfeldt T

doi

10.1016/0014-2999(94)90468-5

subject

Has Abstract

pub_date

1994-03-21 00:00:00

pages

291-4

issue

3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(94)90468-5

journal_volume

254

pub_type

杂志文章
  • Comparative effects of K+ channel blockade on the vasorelaxant activity of cromakalim, pinacidil and nicorandil.

    abstract::Three agents with K+ channel blocking activity, procaine, 4-aminopyridine (4-AP) and tetraethylammonium (TEA), were tested for inhibition of vasorelaxation and 86Rb+ efflux induced by cromakalim (BRL 34915), pinacidil and nicorandil in rabbit isolated mesenteric artery. The potency order for inhibition of vasorelaxati...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90728-5

    authors: Wilson C,Coldwell MC,Howlett DR,Cooper SM,Hamilton TC

    更新日期:1988-08-02 00:00:00

  • Peripheral kappa 1-opioid receptor-mediated analgesia in mice.

    abstract::When injected directly into the tail, U50,488H is a potent analgesic in the tailflick assay (ED50 3.1 micrograms). The analgesic activity is lost if the radiant heat is focused 1 cm away from the site of injection. The kappa 1-opioid receptor antagonist nor-binaltorphimine given systemically reverses the local analges...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(96)00520-1

    authors: Kolesnikov Y,Jain S,Wilson R,Pasternak GW

    更新日期:1996-08-29 00:00:00

  • Exogenous SO2 donor treatment impairs reconsolidation of drug reward memory in mice.

    abstract::Substance-related and addictive disorders (SRADs) are characterized by compulsive drug use and recurrent relapse. The persistence of pathological drug-related memories indisputably contributes to a high propensity to relapse. Hence, strategies to disrupt reconsolidation of drug reward memory are currently being pursue...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2021.173911

    authors: Rulan D,Zhenbang Y,Yipu Z,Yuan G,Galaj E,Xiaorui S,Wenshuya L,Jiaqi L,Yan Z,Chang Y,Xi Y,Li S,Yixiao L,Haishui S

    更新日期:2021-01-24 00:00:00

  • The alpha 1-adrenoceptor is inactivated by alterations in membrane phospholipids.

    abstract::The influence of the membrane environment on the alpha 1-adrenoceptor has been investigated by examining the effect of phospholipase digestion on the binding of [3H]prazosin to aortic and hepatic membranes. Membrane digestion by phospholipase A2 and phospholipase C was found to markedly reduce prazosin binding to the ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(92)90079-b

    authors: Shreeve SM,Valliere JE

    更新日期:1992-05-12 00:00:00

  • Modulation of the release of endogenous gamma-aminobutyric acid by cannabinoids in the guinea pig ileum.

    abstract::Interactions between cannabinoid CB(1) and GABA receptors and ligands were investigated in the myenteric plexus-longitudinal muscle of the guinea pig ileum. Electrically evoked contractions of the myenteric plexus-longitudinal muscle were inhibited by the cannabinoid receptor agonist CP55,940 ((-)-cis-3-[2-Hydroxy-4-(...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)01530-8

    authors: Begg M,Molleman A,Parsons M

    更新日期:2002-01-02 00:00:00

  • Structure-activity relationships of an endothelin ETA receptor antagonist, 50-235, and its derivatives.

    abstract::27-O-Caffeoyl myricerone (50-235) is a nonpeptide endothelin receptor antagonist which is highly selective for the endothelin ETA receptor subtype. In order to determine which functional groups in 50-235 are essential for its activity, we examined the potencies of 50-235 and its derivatives to inhibit [125I]endothelin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(93)90081-j

    authors: Mihara S,Sakurai K,Nakamura M,Konoike T,Fujimoto M

    更新日期:1993-10-15 00:00:00

  • Autonomic receptor systems in the failing and aging human heart: similarities and differences.

    abstract::Changes in autonomic receptor systems (alpha- and beta-adrenoceptors and muscarinic receptors) were compared in the aging and failing human heart. In both settings responsiveness of beta-adrenoceptors and all other receptor systems that evoke their effects via cyclic AMP accumulation was diminished. Muscarinic recepto...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2004.07.022

    authors: Brodde OE,Leineweber K

    更新日期:2004-10-01 00:00:00

  • Neferine, an alkaloid ingredient in lotus seed embryo, inhibits proliferation of human osteosarcoma cells by promoting p38 MAPK-mediated p21 stabilization.

    abstract::Identification of natural products that have antitumor activity is invaluable to the chemoprevention and therapy of cancer. The embryos of lotus (Nelumbo nucifera) seeds are consumed in beverage in some parts of the world for their presumed health-benefiting effects. In this report we studied the effects of neferine, ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.12.035

    authors: Zhang X,Liu Z,Xu B,Sun Z,Gong Y,Shao C

    更新日期:2012-02-29 00:00:00

  • Antagonism by tubocurarine and verapamil of the regenerative acetylcholine release from mouse motor nerve.

    abstract::The role of presynaptic acetylcholine receptors and Ca2+ channels in the regenerative acetylcholine release was studied in the cut muscle preparation of mouse phrenic nerve hemidiaphragm. The regenerative release shown as a prolonged endplate depolarization was evoked by stimulation of the nerve with a train of pulse ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90598-0

    authors: Hong SJ,Chang CC

    更新日期:1989-03-14 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

  • Genetical differences in sensitivity to tremorine and oxotremorine in mice.

    abstract::Male mice from 14 strains were injected i.p. with tremorine (3.0 mg/kg) or oxotremorine (0.15 or 0.1 mg/kg). Large inter-strain differences in the degree and duration of the subsequent hypothermia were noted. 2 strains, BALB/c and Simpson, were particularly sensitive to the hypothermic effect of oxotremorine. The offs...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(78)90226-1

    authors: Lush IE,Andrews KM

    更新日期:1978-05-01 00:00:00

  • Epidermal growth factor protects mouse ileal mucosa from Triton X-100-induced injury.

    abstract::Luminal exposure of mouse ileal mucosal sheets in vitro to 0.3% Triton X-100 for 10 min resulted in a 45.3 +/- 4.4% decrease in tissue resistance (Rt). Luminal pretreatment of tissue with epidermal growth factor (EGF, 30 nM) reduced the Triton X-100-induced decrease in Rt to 10.2 +/- 3.5%. This effect of luminal EGF w...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(96)00186-0

    authors: Rao R,Porreca F

    更新日期:1996-05-15 00:00:00

  • Activation of KATP channels increases anticancer drug delivery to brain tumors and survival.

    abstract::Several anticancer drugs are ineffective against brain tumor and do not impact patient survival because they fail to cross the blood-brain tumor barrier (BTB) effective levels. One such agent temozolomide is commonly used in brain tumor patients, which works better when combined with radiation or other anticancer agen...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.10.056

    authors: Ningaraj NS,Sankpal UT,Khaitan D,Meister EA,Vats T

    更新日期:2009-01-14 00:00:00

  • Possible mechanism of action of diazepam as an adenosine potentiator.

    abstract::Diazepam (10(-5)-3 X 10(-4) M) selectively enhanced the negative inotropic responses of guinea-pig atria and the relaxation of guinea-pig taenia coli caused by adenosine and ATP. In the atria, the effect of 2-chloroadenosine, a stable analog of adenosine, was not affected by diazepam. Segments of guinea-pig atria or t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90346-2

    authors: Moritoki H,Fukuda H,Kotani M,Ueyama T,Ishida Y,Takei M

    更新日期:1985-07-11 00:00:00

  • Salidroside stimulated glucose uptake in skeletal muscle cells by activating AMP-activated protein kinase.

    abstract::In the present study, we reported the metabolic effects of salidroside, one of the active components of Rhodiola Rosea, on skeletal muscle cells. Salidroside dose-dependently stimulated glucose uptake in differentiated L6 rat myoblast cells. Inhibitor of AMP-activated protein kinase (AMPK) by pretreating the cells wit...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.04.036

    authors: Li HB,Ge YK,Zheng XX,Zhang L

    更新日期:2008-07-07 00:00:00

  • Behavioural and biochemical changes following chronic administration of L-dopa to rats.

    abstract::Rats were given powdered diet containing L-DOPA (together with the peripheral decarboxylase inhibitor carbidopa) for a period of 6 months. The estimated daily intake was in the range 20-30 mg/kg. Initially, at 1 week and 1 month, L-DOPA-fed rats exhibited enhanced spontaneous locomotor activity, but this fell to withi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90626-4

    authors: Pycock C,Dawbarn D,O'Shaughnessy C

    更新日期:1982-04-23 00:00:00

  • BW-A522 blocks adenosine A3 receptor-mediated hypotensive responses in the rat.

    abstract::The effects of 3-(3-iodo-4-aminobenzyl)-8-(4-oxyacetate)-1-propylxanthine (I-ABOPX; BW-A522), which has nanomolar affinity for the recently cloned human and sheep adenosine A3 receptor, on the putative A3 receptor mediated hypotensive response to N6-2-(4-aminophenyl)ethyl adenosine (APNEA) in the rat have been investi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90604-1

    authors: Fozard JR,Hannon JP

    更新日期:1994-02-03 00:00:00

  • Reduced contractile function after balloon denudation of rat carotid arteries.

    abstract::In rat carotid arteries isolated 2 weeks after balloon denudation, a significant neointima developed with little change in medial size. Associated with this neointimal hyperplasia was a marked decrease in contraction to various agents including angiotensins I and II, big endothelin-1, endothelin-1, norepinephrine, phe...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90610-6

    authors: Antonaccio MJ,Normandin D,Ferrer P

    更新日期:1994-04-11 00:00:00

  • Aporphines. 15. Action of aporphine alkaloids on dopaminergic mechanisms in rat brain.

    abstract::Of eleven aporphine analogues tested on striatal adenylate cyclase only (-)-apomorphine and (+/-)-N-n-propyl-norapomorphine (+/-(NPA)) were effective in stimulating the cyclase from rat brain. Inactive compounds included (+/-)-isoapomorphine, (-)-1,2-dihydroxyaporphine and (+/-)-10-hydroxy-N-n-propylnoraporphine. (+)-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(76)90302-2

    authors: Miller RJ,Kelly PH,Neumeyer JL

    更新日期:1976-01-01 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

  • Chelerythrine and bisindolylmaleimide I prolong cardiac action potentials by protein kinase C-independent mechanism.

    abstract::Effects of chelerythrine and bisindolylmaleimide I on action potential duration and on voltage-activated K(+) and Ca(2+) currents in rat ventricular myocytes were studied using perforated patch-clamp technique. The action potentials were markedly prolonged after application of 20 microM chelerythrine or 100 nM bisindo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)01541-3

    authors: Voutilainen-Myllylä S,Tavi P,Weckström M

    更新日期:2003-04-11 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

  • H89 (N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide) induces reduction of myosin regulatory light chain phosphorylation and inhibits cell proliferation.

    abstract::H89 (N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide) is a compound characterized in vitro as a potent and selective inhibitor of protein kinase A (PKA). In this study, we found that H89 reduced the phosphorylation of the myosin regulatory light chain (MRLC) at Thr-18/Ser-19 and induced disassembly of stre...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.05.029

    authors: Umeda D,Yamada K,Tachibana H

    更新日期:2008-08-20 00:00:00

  • Adaptation of cortical NMDA receptors by chronic treatment with specific serotonin reuptake inhibitors.

    abstract::Glycine displaces [3H]CGP-39653 ([3H]D,L-(E)-2-amino-4-propyl-5-phosphono-3-pentenoic acid) binding to the glutamate recognition site with both high and low affinity. We reported previously that chronic treatment with antidepressants reduced the proportion of high to low affinity sites, or, even eliminated the high af...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)01589-6

    authors: Nowak G,Legutko B,Skolnick P,Popik P

    更新日期:1998-01-26 00:00:00

  • Interaction between 5-hydroxytryptamine and other vasoconstrictor substances in the isolated femoral artery of the rabbit; effect of ketanserin (R 41 468).

    abstract::Experiments were designed to determine whether or not ketanserin (R 41 468) antagonizes the augmentation by 5-hydroxytryptamine of contractions evoked in isolated arteries by non-adrenergic vasoconstrictor substances. Rings of rabbit femoral arteries were studied under isometric conditions in organ chambers filled wit...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90130-3

    authors: Van Nueten JM,Janssen PA,De Ridder A,Vanhoutte PM

    更新日期:1982-02-05 00:00:00

  • Neurotoxic effect of prenatal exposure to MPTP on the dopaminergic systems of the marmoset brain.

    abstract::MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) was incidentally administered to pregnant marmosets during the whole gestational period, except for the last 15 days before term. The infant monkeys were killed 5 months after birth, and dopamine and its metabolites were measured in the striatum and the nucleus accum...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90873-3

    authors: Pérez-Otaño I,Oset C,Trinidad Herrero M,Luquin MR,Kupsch A,Oertel W,Obeso JA,Del Río J

    更新日期:1992-07-07 00:00:00

  • WISP1 overexpression promotes proliferation and migration of human vascular smooth muscle cells via AKT signaling pathway.

    abstract::Proliferation and migration of vascular smooth muscle cells (VSMCs) play crucial roles in the development of vascular restenosis. Our previous study showed that CCN4, namely Wnt1 inducible signaling pathway protein 1 (WISP1), significantly promotes proliferation and migration of rat VSMCs, but its mechanism remains un...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.06.027

    authors: Lu S,Liu H,Lu L,Wan H,Lin Z,Qian K,Yao X,Chen Q,Liu W,Yan J,Liu Z

    更新日期:2016-10-05 00:00:00

  • BHT-920 and LY-171555 (quinpirole) have similar affinities for striatal D-2 dopamine receptors, and similar affinities for striatal D-1 dopamine receptors.

    abstract::The affinity of LY-171555 (quinpirole) and BHT-920 for both states of rat striatal dopamine D-1 and D-2 receptors was determined. Although these drugs have different pharmacological effects in experimental animals, we found that they had similar affinities for both D-1 and D-2 receptors. ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90072-1

    authors: Ferré S,Guix T,Sallés J,Cuffí L,Badia A,Casas M

    更新日期:1989-07-18 00:00:00

  • Inhibition of the P-glycoprotein- and multidrug resistance protein-mediated efflux of anthracyclines and calceinacetoxymethyl ester by PAK-104P.

    abstract::Multidrug resistance phenotype in mammalian cells is often correlated with overexpression of P-glycoprotein or Multidrug Resistance-Associated protein (MRP(1)). Both proteins are energy-dependent drug efflux pumps that efficiently reduce the intracellular accumulation and hence the cytotoxicity of many natural cytotox...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00047-9

    authors: Marbeuf-Gueye C,Salerno M,Quidu P,Garnier-Suillerot A

    更新日期:2000-03-17 00:00:00

  • Involvement of the strychnine-sensitive glycine receptor in the anxiolytic effects of GlyT1 inhibitors on maternal separation-induced ultrasonic vocalization in rat pups.

    abstract::Several studies have shown that glycine transporter 1 (GlyT1) inhibitors have anxiolytic actions. There are two types of glycine receptor: the strychnine-sensitive glycine receptor (GlyA) and the strychnine-insensitive glycine receptor (GlyB); however, which receptor is the main contributor to the anxiolytic actions o...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.11.024

    authors: Komatsu H,Furuya Y,Sawada K,Asada T

    更新日期:2015-01-05 00:00:00