Search results for "Benzazepine"
showing 10 items of 43 documents
Effects of SCH 23390, Raclopride, and Haloperidol on Morphine Withdrawal-Induced Aggression in Male Mice
1999
Abstract RODRIGUEZ-ARIAS, M., J. PINAZO, J. MINARRO AND L. STINUS. Effects of SCH 23390, raclopride, and haloperidol on morphine withdrawal-induced aggression in male mice. PHARMACOL BIOCHEM BEHAV 64(1) 123–130, 1999.—Dopamine seems to play a very important role in aggressive behavior observed in morphine withdrawal. The effect of SCH 23390 (0.5 mg/kg), raclopride (0.3 mg/kg), and haloperidol (0.1 mg/kg) on morphine withdrawal-induced aggression has been studied in this work. Mice were rendered dependent by a daily injection of morphine (2.5 mg/kg) for 14 days. Three different experiments were carried out with the objective to evaluate the antiaggressive effect of the dopamine antagonists o…
Modification of depressant and disinhibitory action of flurazepam during short term treatment in the rat
1972
Employing a fixed-interval schedule of reinforcement (temporal discrimination), alternated punished (fixed-ratio) and unpunished (variable-ratio) schedules of reinforcement, a Conditioned Avoidance Response, and studying its interaction with Pentobarbital on general anaesthesia, it has been shown that flurazepam hydrochloride after a single treatment induces very intense depressant effects and slight disinhibitory effects. Short term treatment at longer than daily intervals reduces the depressant effect and unmasks the disinhibitory effect. The phenomenon is probably caused by selective tolerance concerning the depressant action. The results are discussed from the point of view of the signi…
Enantioselective syntheses of dopaminergic (R)- and (S)-benzyltetrahydroisoquinolines.
2001
Optically pure (1S,R)- and (1R,S)-benzyltetrahydroisoquinolines (BTHIQs), 12a,b as the major diastereomers, were prepared by stereoselective reduction of the isoquinolinium salt possessing (R)- and (S)-phenylglycinol as the chiral auxiliary, respectively. The absolute configurations of (1S,R)-13a hydrochloride (O-debenzoylated derivative from 12a) and (1R,S)-12b diastereomers were unambiguously determined by single-crystal X-ray analysis. Reductive removal of the chiral auxiliary group, subsequent N-propylation, and cleavage of the methylenedioxy group furnished the optically active catecholamines (1S)-16a and (1R)-16b in good overall yield. We have separately prepared for the first time pa…
Sex differences in escape-avoidance response in mice after acute administration of raclopride, clozapine, and SCH 23390.
1998
Sex differences in the effects of haloperidol in the escape-avoidance response in mice have previously been found in various studies carried out in our laboratory. Males were more affected than females by the disruptive effects of this neuroleptic. The work described herein extended the study of these sex differences to raclopride, clozapine, and SCH 23390, using several doses of each drug in acute administration. The results showed dose-dependent sex differences in the deteriorating effects of these dopamine antagonists in the escape-avoidance response. Male mice were more affected by the inhibitory effects of these drugs, showing fewer escape responses and more nonresponses than females. …
Effect of verapamil and diltiazem on isolated gastro-oesophageal sphincter of the rat
1985
Abstract The effect of verapamil and diltiazem on the contraction induced by agonists on the rat lower oesophageal sphincter in-vitro has been studied. Both calcium entry blockers inhibited the contractile response to acetylcholine, carbachol and KCl. The potency of the inhibitory action was diltiazem > verapamil. The results give substance to the use of calcium entry blockers in the treatment of oesophageal spasm.
Sensitization to the rewarding effects of morphine depends on dopamine
2005
The influence of dopamine (DA) on sensitization to the rewarding effects of morphine was evaluated. The effects of pre-treatment with saline or morphine plus naloxone, CGS 10746B, haloperidol, SCH 23390 and raclopride, on the place conditioning induced by 2 mg/kg morphine were evaluated. This dose was ineffective in saline pre-treated animals but induced a clear conditioned place preference in mice pre-treated with morphine, CGS 10746B or haloperidol. Conversely, animals pre-treated with morphine plus naloxone, CGS 10746B, SCH 23390, raclopride and the high dose of haloperidol did not acquire place preference. Our results demonstrated that DA release and subsequent DA D1 and D2 receptor act…
Role of dopamine neurotransmission in the long-term effects of repeated social defeat on the conditioned rewarding effects of cocaine
2016
Numerous studies report that social defeat stress alters dopamine (DA) neurotransmission in several areas of the brain. Alterations of the mesolimbic dopaminergic pathway are believed to be responsible for the increased vulnerability to drug use observed as a result of social stress. In the present study, we evaluated the influence of DA receptors on the long-term effect of repeated social defeat (RSD) on the conditioned rewarding and reinstating effects of cocaine. For this purpose, the D1R antagonist SCH 23390 and the D1R antagonist raclopride were administered 30 min before each social defeat and a cocaine-induced CPP procedure was initiated three weeks later. The expression of the D1R a…
Hippocampal dopamine receptors modulate the motor activation and the increase in dopamine levels in the rat nucleus accumbens evoked by chemical stim…
2005
A number of studies have shown that chemical stimulation (using N-methyl-D-aspartate (NMDA) infusions) or electrical stimulation of the ventral hippocampus (VH) elicits locomotor activation and sustained increases in nucleus accumbens (NAc) dopamine (DA) levels in rodents. How DA neurotransmission in NAc is involved in these effects has also been well established. However, the modulatory role of the DA receptors located in VH is not yet fully understood. The purpose of this study was to characterize the role played by VH D1 and D2 subtype receptors in both the locomotor activation and NAc DA increases induced by NMDA stimulation of the VH. This was assessed by studying how retrodialysis app…
Hippocampal dopamine receptors modulate cFos expression in the rat nucleus accumbens evoked by chemical stimulation of the ventral hippocampus
2005
Recently, we have shown that D1 and D2 receptors in the ventral hippocampus (VH) modulate both the locomotor activation and the increase in dopamine (DA) levels in the rat nucleus accumbens (NAc) induced by NMDA stimulation of the VH. In the present study we analyze the possible role of VH D1 and D2 receptors in the modulation of the cFos expression in NAc (core and shell subregions) and in dorsal striatum. This was assessed by immunohistochemical analysis of cFos expression in the rat brains after retro-dialysis application of NMDA (50mM, 10 min) into VH, in absence and in presence of either the D1/D5 receptor antagonist SCH 23390 (100 and 250 microM, 60 min) or the D2 receptor antagonist …
Impact of ''off-label'' use of ivabradine on exercise capacity, gas exchange, functional class, quality of life, and neurohormonal modulation in pati…
2010
Background: Epidemiologic studies indicate that elevated heart rate (HR) is an independent risk factor for mortality and morbidity in patients (pts) with chronic heart failure (CHF). Clinical trials with b-blockers suggest that HR reduction is an important mechanism of their benefit in pts with stable CHF. Pharmacologic inhibition of the If current now provides the opportunity of pure HR reduction. The purpose of this study was to evaluate the impact of ‘‘Off-Label’’ use of ivabradine on exercise capacity, gas exchange, functional class, quality of life, and neurohormonal modulation in pts with ischemic CHF. Methods: Between January 2008 and June 2008, a graded maximal exercise test with re…