Search results for "Benzazepines"
showing 10 items of 38 documents
Influence of pH on the benzodiazepine-human serum albumin complex. Circular dichroism studies.
1974
The influence of pH on the binding of benzodiazepine derivatives to HSA was studied by circular dichroism measurements and by gel filtration. The binding of nearly all benzodiazepines is increased by rising the pH from 6.60 to 8.20. For flurazepam, clonazepam, and nitrazepam this increase in binding is due to an increase of the affinities, while for the other substances the affinity remains constant and the number of binding sites is increased from one to two. The changes in binding of the benzodiazepines by rising the pH are explained by a cationic amino acid residue near or at the benzodiazepine binding site of the HSA molecule. This second binding site is not detectable by circular dichr…
Heart rate control with oral ivabradine in computed tomography coronary angiography: a randomized comparison of 7.5 mg vs 5 mg regimen.
2013
Background: Heart rate (HR) reduction is essential to achieve optimal image quality and diagnostic accuracy with computed tomography coronary angiography (CTCA). Administration of oral ivabradine seems to be more effective than beta-blockade in reducing HR in patients referred for CTCA. Methods: Two-hundred-fifty-nine consecutive patients referred for CTCA were prospectively enrolled. Patients not receiving beta-blocker at baseline (group 1) and those with beta-blocker therapy (group 2) were enrolled in the study. Each group was randomized into 3 parallel arms with 1:1:1 allocation. Patients who did not receive beta-blocker at baseline: underwent CTCA without beta blocker (n=49), and receiv…
Production of specific antibodies and development of a non-isotopic immunoassay for carbamazepine by the carbonyl metallo-immunoassay (CMIA) method.
1995
Abstract As part of our ongoing work to extend the range of applications of the non-isotopic carbonyl metalloimmunoassay (CMIA), previously developed in our laboratory, we describe here the first CMIA study of carbamazepine. The CMIA method uses a metal carbonyl complex as a non-isotopic tracer, and in this case we chose to employ the dicobalt hexacarbonyl moiety (Co2(CO)6) attached to an alkyne. Two organometallic tracers, 3 and 7 , were synthesized, differentiated by the nature and length of the spacer arm of the Co2(CO)6 moiety. Two different coupling methods were subsequently used to synthesize the immunogens 1 and 2, the first one used a carbodiimide, while the second, employed dimethy…
Synthesis and characterization of biotinylated and photoactivatable neuroleptics. Novel bifunctional probes for dopamine receptors
1992
Abstract We have synthesized and characterized a series of novel derivatives of established antagonists of the neurotransmitter dopamine, i.e. butyrophenones, hexahydrocarbolines and phenothiazenes. All derivatives were biotinylated, some of them carried an additional (photoactivatable) azido group. In the case of butyrophenones, the structural modifications were introduced at the aliphatic keto group and/or the heterocyclic ring system, both modifications resulting in significant decreases in binding affinity to dopamine D 2 and dopamine D 1 receptor subtypes. Biotinylation of hexahydrocarbolines significantly increased their binding affinity to D 1 receptors, with the affinity for D 2 rec…
Incremental value and safety of oral ivabradine for heart rate reduction in computed tomography coronary angiography
2012
Background: Heart rate (HR) reduction is essential to achieve optimal image quality and diagnostic accuracy with computed tomography coronary angiography (CTCA). Administration of ivabradine could be an attractive alternative to beta-blockade to reduce HR. Methods: One-hundred-twenty-three patients referred for CTCA were prospectively enrolled. Patients were divided in two groups depending on the absence or presence of chronic beta-blockade treatment. Within the two groups patients were randomized to either no additional premedication or oral ivabradine for 5 days prior to CTCA. In presence of chronic beta-blockade therapy it was shifted to atenolol 50 mg twice a day for 5 days prior to CTC…
Effects of risperidone and SCH 23390 on isolation-induced aggression in male mice.
1998
In this study, the antiaggressive effects of risperidone and SCH 23390 have been explored. Using the paradigm of isolation-induced aggression, 150 albino male mice of the OF1 strain were allocated to control and experimental groups which received three doses of risperidone (0.01, 0.05 and 0.1 mg/kg) or two doses of SCH 23390 (0.05 and 0.1 mg/kg). Only the highest doses of risperidone decreased threat and attack behaviours but all doses significantly impaired motor behaviour. SCH 23390 decreased attack with the two doses used and also produced significant increases in immobility. Although both antipsychotics are antiaggressive, this action seems to be more specific in the case of risperidone…
Role of the dopaminergic system in the acquisition, expression and reinstatement of MDMA-induced conditioned place preference in adolescent mice.
2012
Background The rewarding effects of 3,4-methylenedioxy-metamphetamine (MDMA) have been demonstrated in conditioned place preference (CPP) procedures, but the involvement of the dopaminergic system in MDMA-induced CPP and reinstatement is poorly understood. Methodology/Principal Findings In this study, the effects of the DA D1 antagonist SCH 23390 (0.125 and 0.250 mg/kg), the DA D2 antagonist Haloperidol (0.1 and 0.2 mg/kg), the D2 antagonist Raclopride (0.3 and 0.6 mg/kg) and the dopamine release inhibitor CGS 10746B (3 and 10 mg/kg) on the acquisition, expression and reinstatement of a CPP induced by 10 mg/kg of MDMA were evaluated in adolescent mice. As expected, MDMA significantly increa…
Lack of Specific Effects of Selective D1 and D2 Dopamine Antagonists vs. Risperidone on Morphine-Induced Hyperactivity
2000
Abstract RODRIGUEZ-ARIAS, M., I. BROSETA, M. A. AGUILAR AND J. MINARRO. Lack of specific effects of selective D 1 and D 2 dopamine antagonists on morphine-induced hyperactivity. PHARMACOL BIOCHEM BEHAV 66 (1) 189–197, 2000.—In the present study, three different dopamine antagonists were challenged in order to counteract hyperactivity induced by 50 mg/kg of morphine. A wide range of doses of morphine (50, 25, 12.5, 6.25, or 3.12 mg/kg) were evaluated on spontaneous locomotor activity. A significant increase was observed only with the two higher doses tested (25 and 50 mg/kg). No decrease was found with any of the doses used at any period of time. After analyzing doses of SCH 23390 (0.5, 0.1,…
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…