Lack of dopamine supersensitivity in rats after chronic administration of blonanserin: Comparison with haloperidol.

Abstract:

:Long-term treatment with antipsychotic drugs in patients with schizophrenia can lead to dopamine supersensitivity psychosis. It is reported that repeated administration of haloperidol caused dopamine supersensitivity in rats. Blonanserin is an atypical antipsychotic drug with high affinity for dopamine D2, D3 and serotonin2A receptors. In this study, we investigated whether chronic administration of blonanserin leads to dopamine supersensitivity. Following oral treatment with blonanserin (0.78 mg/kg) or haloperidol (1.1 mg/kg) twice daily for 28 days, the dopamine D2 agonist quinpirole-induced hyperlocomotion test and a dopamine D2 receptor binding assay were conducted. We found that haloperidol significantly enhanced both quinpirole-induced hyperlocomotion and striatal dopamine D2 receptor density in rats. On the other hand, repeated administration of blonanserin had no effect on either locomotor activity or striatal dopamine D2 receptor density. Further, our results show that mRNA levels of dopamine D2 and D3 receptors in several brain regions were unaffected by repeated administration of both agents. In addition, we examined the effect of the dopamine D3 receptor antagonist PG-01037 on development of dopamine supersensitivity induced by chronic haloperidol treatment and showed that PG-01037 prevents the development of supersensitivity to quinpirole in chronic haloperidol-treated rats. Given the higher affinity of blonanserin at dopamine D3 receptors than haloperidol, antagonism of blonanserin at dopamine D3 receptors may play a role in lack of dopamine supersensitivity after chronic administration. The present findings suggest long-term treatment with antipsychotic dose of blonanserin may be unlikely to lead to dopamine supersensitivity.

journal_name

Eur J Pharmacol

authors

Hashimoto T,Baba S,Ikeda H,Oda Y,Hashimoto K,Shimizu I

doi

10.1016/j.ejphar.2018.04.014

subject

Has Abstract

pub_date

2018-07-05 00:00:00

pages

26-32

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(18)30226-7

journal_volume

830

pub_type

杂志文章
  • Desensitization of neurokinin A receptors expressed by B82 fibroblasts.

    abstract::After chronic exposure to neurokinin A, a time-dependent and recoverable desensitization of inositol monophosphate accumulation occurred in B82 fibroblasts transfected with cDNAs encoding for the bovine stomach NK2 receptor. Desensitized cells also showed decreased Ca2+ mobilization. While NK2 receptor antagonists had...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(93)90172-6

    authors: Henderson AK,Roeske WR,Smith TL,Yamamura HI

    更新日期:1993-03-15 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

  • Hydrophilic residues at position 3 highlight unforeseen features of the fMLP receptor pocket.

    abstract::The peptides for-Met-Leu-Tyr-OMe, for-Met-Leu-Glu-OMe, for-Met-Leu-Asp-OMe and for-Met-Leu-Ser-OMe were synthesized to investigate the importance of a hydrophilic side chain of the residue at position 3 on biological activities of human neutrophils. A number of in vitro essays were carried out, including: chemotaxis, ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)01672-8

    authors: Spisani S,Turchetti M,Varani K,Falzarano S,Cavicchioni G

    更新日期:2003-05-23 00:00:00

  • GABA receptor-mediated modulation of 3H-diazepam binding in rat cortex.

    abstract::Three membrane preparations of rat cortex were used to examine the effects of GABA, bicuculline and bicucine on specific 3H-diazepam binding. In the crude synaptosomal fraction, GABA had no effect on either the maximal binding capacity (Bmax) or dissociation constant (KD) of 3H-diazepam binding. Bicuculline and bicuci...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(79)90264-4

    authors: Chiu TH,Rosenberg HC

    更新日期:1979-07-01 00:00:00

  • Pharmacological characterization of urinary bladder smooth muscle contractility following partial bladder outlet obstruction in pigs.

    abstract::Partial bladder outlet obstruction of the pig is considered as a valuable preclinical model for evaluating the profile of compounds for the treatment of bladder overactivity. In this study, we characterized the pharmacological properties of isolated bladder smooth muscle from pigs following partial outlet obstruction ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.12.076

    authors: Milicic I,Buckner SA,Daza A,Coghlan M,Fey TA,Brune ME,Gopalakrishnan M

    更新日期:2006-02-17 00:00:00

  • Protective effects of KW-3635, a novel thromboxane A2 antagonist, in murine traumatic shock.

    abstract::Pentobarbital anesthetized rats subjected to Noble-Collip drum trauma developed a shock state characterized by marked hypotension, increases in plasma cathepsin D (9.6-fold), free amino-nitrogen (4.0-fold), and myocardial depressant factor (5.2-fold) activities, and a survival time of 1.90 +/- 0.23 h. Following the in...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90487-q

    authors: Karasawa A,Taylor PA 3rd,Lefer AM

    更新日期:1990-06-21 00:00:00

  • Dopamine D4 receptors bind inactive (+)-aporphines, suggesting neuroleptic role. Sulpiride not stereoselective.

    abstract::In order to identify new atypical antipsychotic drugs which are more selective for the human dopamine D4 receptor than for the human dopamine D2 (long) receptor, we tested enantiomer pairs of dopamine agonists and dopamine antagonists on the expressed proteins of these cloned receptors. The (+)-aporphines ((+)-N-propy...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90365-o

    authors: Seeman P,Van Tol HH

    更新日期:1993-03-16 00:00:00

  • Effect of NZ-107 on late-phase airway responses and airway hyperreactivity in guinea pigs.

    abstract::The effect of NZ-107 (4-bromo-5-(3-ethoxy-4-methoxybenzylamino)-3(2H)-pyridazinone) on late-phase airway responses and airway hyperreactivity was investigated in the guinea pig. Challenge with inhaled ovalbumin in conscious guinea pigs actively sensitized with inhaled ovalbumin caused triphasic bronchial obstruction, ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90490-h

    authors: Iwama T,Shikada K,Yamamoto A,Sakashita M,Hibi M,Tanaka S

    更新日期:1991-07-09 00:00:00

  • The effect of O-1602, a GPR55 agonist, on the cyclophosphamide-induced rat hemorrhagic cystitis.

    abstract::The goal of our study was to determine whether GPR55 agonists, O-1602, could reverse the cyclophosphamide (CYP)-induced changes in cystometric and inflammatory parameters, indicative of the development of bladder inflammation and overactivity. If confirmed, the stimulation of novel cannabinoid receptor - GPR55, could ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173321

    authors: Wróbel A,Zapała Ł,Zapała P,Piecha T,Radziszewski P

    更新日期:2020-09-05 00:00:00

  • C-fibers, but not the transient potential receptor vanilloid 1 (TRPV1), play a role in experimental allergic airway inflammation.

    abstract::The activation of C-fibers in the airways induces coughing, mucus production and bronchoconstriction, which are also symptoms of airway diseases. In this study, we evaluated the role of the C-fibers and the TRPV1 (transient receptor potential vanilloid 1) receptor in an experimental mouse model of allergic airway infl...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.04.027

    authors: Rogerio AP,Andrade EL,Calixto JB

    更新日期:2011-07-15 00:00:00

  • Effects of the putative lithium mimetic ebselen on pilocarpine-induced neural activity.

    abstract::Lithium, commonly used to treat bipolar disorder, potentiates the ability of the muscarinic agonist pilocarpine to induce seizures in rodents. As this potentiation by lithium is reversed by the administration of myo-inositol, the potentiation may be mediated by inhibition of inositol monophosphatase (IMPase), a known ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173377

    authors: Singh N,Serres F,Toker L,Sade Y,Blackburn V,Batra AS,Saiardi A,Agam G,Belmaker RH,Sharp T,Vasudevan SR,Churchill GC

    更新日期:2020-09-15 00:00:00

  • Effect of yohimbine on the contractile response of the mouse vas deferens to short, low frequency trains of nerve impulses.

    abstract::A study was undertaken to ascertain why in the mouse vas deferens excitatory junction potentials facilitate whereas contractions depress during low frequency stimulation. In a set of contraction studies, where a conditioning stimulus was followed 2 s later by a test stimulus, depression in the first phase of contracti...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90295-x

    authors: Karunanithi S,Lavidis NA,Bennett MR

    更新日期:1994-08-11 00:00:00

  • Ethacrynic acid inhibition of histamine release from rat mast cells: effect on cellular ATP levels and thiol groups.

    abstract::The experiments concerned the effect of ethacrynic acid (0.5 mM) on the adenosine triphosphate (ATP) content of rat mast cells and the effect on histamine release induced by the ionophore A23187 (10 microM). Ethacrynic acid decreased the ATP level of the cells in presence of antimycin A and glucose as well as in prese...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90285-6

    authors: Johansen T

    更新日期:1983-09-02 00:00:00

  • Gabaergic stimulation inhibits central actions of angiotensin II: pressor responses, drinking and release of vasopressin.

    abstract::In conscious rats, intracerebroventricular (i.c.v.) treatment with the GABA agonist muscimol (1-100 ng) suppressed the pressor responses to ANG II (100 ng i.c.v.) in a dose-dependent and reversible fashion. Treatment i.c.v. with GABA (1-500 micrograms) produced a similar but shorter inhibition. Inhibition of endogenou...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90207-8

    authors: Unger T,Bles F,Ganten D,Lang RE,Rettig R,Schwab NA

    更新日期:1983-05-20 00:00:00

  • Characterization of 5-HT1A receptor-mediated [35S]GTPgammaS binding in rat hippocampal membranes.

    abstract::Stimulation of [35S]GTPgammaS binding by serotonin (5-hydroxytryptamine, 5-HT) receptor ligands was characterized in rat hippocampal membranes. The optimized assay contained 30-50 microg protein, 300 microM GDP and 0.1 nM [35S]GTPgammaS, incubated at 37 degrees C for 20 min. At 10 microM, the 5-HT1A receptor agonist R...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)01547-1

    authors: Alper RH,Nelson DL

    更新日期:1998-02-19 00:00:00

  • Potential role of peripheral benzodiazepine receptors in inflammatory responses.

    abstract::This study investigates the anti-inflammatory effects of 1-(2-chlorophenyl)-N-methyl-N(1-methylpropyl)-3-isoquinoline carboxamide and 7-chloro-5-(4-chlorophenyl)-1, 3-dihydro-1-methyl-2-H-1,4-benzodiazepin-2-one in paw oedema induced by carrageenan in mice. Pretreatment (24 h) with both ligands inhibited oedema format...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00745-1

    authors: Torres SR,Nardi GM,Ferrara P,Ribeiro-do-Valle RM,Farges RC

    更新日期:1999-12-03 00:00:00

  • Antiarrhythmic potency of procainamide and N-acetylprocainamide in rabbits.

    abstract::The antiarrhythmic potency of procainamide (PA) and N-acetylprocainamide (NAPA) has been investigated in rabbits using isolated atrial preparations and ouabain-induced ventricular fibrillation in vivo. At concentrations in the range 3 x 10(-5) to 1 x 10(-3) M, both PA and NAPA decreased the maximum following frequency...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(78)90373-4

    authors: Minchin RF,Ilett KF,Paterson JW

    更新日期:1978-01-01 00:00:00

  • Effects of the calmodulin inhibitor, trifluoperazine, on membrane potentials and slow action potentials of cultured heart cells.

    abstract::The effects of an inhibitor of calmodulin, trifluoperazine (TFP), were determined on the electrical activity of cultured cell reaggregates derived from chick embryonic hearts (15-day-old). The cells exhibited naturally occurring slowly rising action potentials (APs) having a maximum rate of rise (+Vmax) of less than 3...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90645-9

    authors: Bkaily G,Sperelakis N,Eldefrawi M

    更新日期:1984-10-01 00:00:00

  • CNS site of antiarrhythmic action of diphenylhydantoin (DPH) in the cat.

    abstract::Diphenylhydantoin (DPH) is known to be a potent anticonvulsant agent, useful in treating and preventing grand mal seizures. More recently, DPH was reported also to be a potent antiarrhythmic agent acting by means of a depressant action on the heart. The present experiments demonstrated that DPH has also a potent antia...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(75)90078-3

    authors: Lisander B,Jaju B,Wang SC

    更新日期:1975-03-01 00:00:00

  • Inhibition by nitric oxide and nitric oxide-producing vasodilators of DNA synthesis in vascular smooth muscle cells.

    abstract::Effects of nitric oxide (NO) and NO-producing vasodilators such as glyceryl trinitrate and sodium nitroprusside were tested on DNA synthesis in the clonal rat aortic smooth muscle cells, RACS-1. DNA synthesis was estimated by [3H]thymidine incorporation to DNA. NO and NO-producing vasodilators inhibited the DNA synthe...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(90)90031-r

    authors: Nakaki T,Nakayama M,Kato R

    更新日期:1990-12-15 00:00:00

  • Somatostatin receptor subtype-4 agonist NNC 26-9100 decreases extracellular and intracellular Aβ₁₋₄₂ trimers.

    abstract::Soluble amyloid β-protein (Aβ) oligomers are primary mediators of synaptic dysfunction associated with the progression of Alzheimer's disease. Such Aβ oligomers exist dependent on their rates of aggregation and metabolism. Use of selective somatostatin receptor-subtype agonists have been identified as a potential mean...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.03.020

    authors: Sandoval KE,Farr SA,Banks WA,Crider AM,Morley JE,Witt KA

    更新日期:2012-05-15 00:00:00

  • Role of protein kinase C in the endothelin-induced contraction in the rabbit saphenous vein.

    abstract::The role of protein kinase C in the endothelin-induced contraction was examined in the isolated rabbit saphenous vein in which endothelin-1, endothelin-3, sarafotoxin S6c and IRL 1620 (succinyl-[Glu9,Ala11,15]endothelin-1-(8-21))-induced contraction at the threshold concentrations of 0.1-1 pM. A selective inhibitor of...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00542-0

    authors: Sudjarwo SA,Karaki H

    更新日期:1995-12-27 00:00:00

  • Various GABA-mimetic drugs differently affect cocaine-evoked hyperlocomotion and sensitization.

    abstract::To substantiate the notion that cocaine behavioral effects may be influenced by gamma-aminobutyric acid (GABA) neurotransmission male Wistar rats were injected with gabapentin (a cyclic GABA analogue), tiagabine (a GABA reuptake inhibitor), or vigabatrin (a GABA transaminase inhibitor) before acute or repeated treatme...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.05.011

    authors: Filip M,Frankowska M,Gołda A,Zaniewska M,Vetulani J,Przegaliński E

    更新日期:2006-07-17 00:00:00

  • SNHG9, delivered by adipocyte-derived exosomes, alleviates inflammation and apoptosis of endothelial cells through suppressing TRADD expression.

    abstract::Exosomes are membrane-derived vesicles and play a critical role in cell signaling by transferring RNAs and proteins to target cells through fusion with the cell membrane. Long non-coding RNA-small nucleolar RNA host gene 9 (lncRNA-SNHG9) was proven to be an important element in lncRNA-mRNA interaction networks during ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.172977

    authors: Song Y,Li H,Ren X,Li H,Feng C

    更新日期:2020-04-05 00:00:00

  • Adenosine triphosphate-evoked vascular changes in human skin: mechanism of action.

    abstract::Adenosine triphosphate (ATP), adenosine diphosphate (ADP), adenosine monophosphate (AMP), adenosine, adenine and inosine were injected intradermally into the backs of human volunteers. ATP, ADP and AMP evoked weal and flare responses in the skin in a dose dependent manner. The rank order of potency was ATP greater tha...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(81)90110-2

    authors: Coutts AA,Jorizzo JL,Eady RA,Greaves MW,Burnstock G

    更新日期:1981-12-17 00:00:00

  • Nicorandil prevents doxorubicin-induced human umbilical vein endothelial cell apoptosis.

    abstract::Nicorandil is an adenosine triphosphate-sensitive potassium channel opener with additional antioxidant properties. Doxorubicin (DOX) is an anticancer drug that exerts oxidation-mediated adverse cardiovascular effects. This study examined the effects of nicorandil on DOX-induced cytotoxicity in human umbilical vein end...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2019.172542

    authors: Chen CC,Hong HJ,Hao WR,Cheng TH,Liu JC,Sung LC

    更新日期:2019-09-15 00:00:00

  • Mu- and kappa-opioid receptor agonists produce peripheral inhibition of neurogenic plasma extravasation in rat skin.

    abstract::Extravasation elicited in rat skin by antidromic electrical stimulation of the saphenous nerve was dose dependently inhibited by the intravenous (i.v.) application of the mu-opioid receptor agonists, morphine and [D-Ala2,Me-Phe4,Gly-ol5]enkephalin (DAGO), and the kappa-opioid receptor agonists (-)-U 50488H, (-)-ICI 19...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90233-8

    authors: Barber A

    更新日期:1993-05-12 00:00:00

  • Organ selectivity of hexahydrosiladifenidol in blocking pre- and postjunctional muscarinic receptors studied in guinea-pig ileum and rat heart.

    abstract::Pre- and postjunctional pA2 values of the muscarinic antagonist hexahydrosiladifenidol were determined with guinea-pig ileum and rat heart. Hexahydrosiladifenidol did not discriminate between pre- and postjunctional receptors within the same organ but was more potent on the ileum (20-80 times) than on the heart. It is...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90352-8

    authors: Fuder H,Kilbinger H,Müller H

    更新日期:1985-07-11 00:00:00

  • Effect of N,N-dimethyl-p-methoxyphenylethylamine on blood pressure and brain catecholamines in DOCA-saline hypertensive rats.

    abstract::Intraperitoneal and intraventricular injections of N,N-dimethyl-p-methoxyphenyl ethylamine (PMPEA) decreased blood pressure in conscious DOCA-saline hypertensive rats. Bilateral injection of this agent into the nucleus tractus solitarii (NTS) of anaesthetized normotensive rats also caused a decrease in blood pressure....

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90472-1

    authors: Shalita B,Versteeg DH,De Jong W

    更新日期:1982-11-19 00:00:00

  • Enalapril improves impairment of SERCA-derived relaxation and enhancement of tyrosine nitration in diabetic rat aorta.

    abstract::We investigated the involvement of angiotensin II and vascular smooth muscle sarco/endoplasmic reticulum Ca(2+)-ATPase (SERCA) function in the impaired NO-induced relaxation seen in established streptozotocin-induced diabetes. Plasma angiotensin II levels, which were elevated in untreated diabetic rats (vs age-matched...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.11.026

    authors: Taguchi K,Kobayashi T,Hayashi Y,Matsumoto T,Kamata K

    更新日期:2007-02-05 00:00:00