Drugs online research references
J Clin Psychiatry. 1990 Dec;51 Suppl B:37-9.
The electrocardiogram as a tool for therapeutic monitoring: a critical analysis.
Guy S, Silke B.
Department of Therapeutics and Pharmacology, Queen's University of Belfast, Northern Ireland.
The authors review the scientific value of electrocardiographic studies and discuss the limitations that arise from variability in technology and in standards of recording and interpretation. A consistent recording procedure and objective assessment using standardized diagnostic criteria are required, particularly in multicenter studies. Tricyclic antidepressants depress cardiac conduction at therapeutic concentrations; therefore a comparison with the electrocardiographic profile of sertraline, a specific serotonin reuptake inhibitor with antidepressant activity, was made. In four studies, sertraline was compared with placebo, with amitriptyline or placebo, and with amitriptyline alone. There were decreases in RR interval and increases in PR, QRS, and QTC intervals with amitriptyline but no effect with sertraline. Thus, sertraline had no demonstrable effects on intraventricular conduction or electrocardiographic time intervals.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2258381&dopt=Abstract
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J Pharmacol Exp Ther. 1990 May;253(2):833-40.
Antidepressant actions on brain noradrenergic neurons.
Valentino RJ, Curtis AL, Parris DG, Wehby RG.
Department of Pharmacology, George Washington University Medical Center, Washington, D.C.
Corticotropin-releasing factor (CRF), the hormone responsible for adrenocorticotropin release during stress, is thought to be hypersecreted in depression. Because recent studies suggest that CRF may serve as a neurotransmitter in the major noradrenergic nucleus, locus coeruleus (LC), it was hypothesized that antidepressants interfere with the putative neurotransmitter role of CRF in the LC by either: 1) decreasing release of CRF; 2) pharmacologically antagonizing CRF; or 3) functionally antagonizing CRF by producing effects on LC cells that oppose these of CRF. In order to test this hypothesis, the effects of acute and chronic administration of two antidepressants, a norepinephrine re-uptake inhibitor (desmethylimipramine, DMI) and a serotonin re-uptake inhibitor (sertraline, SER), on LC spontaneous discharge, LC sensory evoked discharge, LC activation by a stressor and LC activation by CRF, were compared in halothane-anesthetized rats. Acute i.v. administration of DMI decreased both LC spontaneous discharge and discharge evoked by repeated sciatic nerve stimulation. In contrast, acute i.v. SER administration decreased only evoked LC discharge rate. Chronic DMI administration (10.0 mg/kg/day, i.p., 21 days) resulted in tolerance to its effects on spontaneous and sensory-evoked LC discharge. However, chronic DMI administration attenuated LC activation by hemodynamic stress, which is thought to require CRF release. LC activation by intracerebroventricular CRF was not altered in the chronic DMI rats. In contrast to DMI, chronic SER (10 mg/kg/day, i.p., 21 days) did not alter LC activation by either stress of CRF. However, the response of LC cells to repeated sciatic nerve stimulation was somewhat enhanced in chronic SER rats. This is an effect that is opposite that produced by CRF.(ABSTRACT TRUNCATED AT 250 WORDS)
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2338658&dopt=Abstract
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Int J Rad Appl Instrum [A]. 1989;40(2):147-51.
The radiosynthesis of [N-methyl-11C]-sertraline.
Lasne MC, Pike VW, Turton DR.
MRC Cyclotron Unit, Hammersmith Hospital, London, U.K.
[N-methyl-11C]Sertraline, a potential agent for the study of the serotonergic system in vivo with positron emission tomography, was prepared by N-methylation of the corresponding norcompound with [11C]iodomethane, which was itself prepared from cyclotron-produced [11C]carbon dioxide. Under the best conditions found [norsertraline free base (20 mM) in DMF (0.70 mL), 120 degrees C for 8 min] [N-methyl-11C]-sertraline can be prepared in 43% radiochemical yield from [11C]iodomethane (decay-corrected), corresponding to 20% overall radiochemical yield from [11C]carbon dioxide (decay-corrected), with high specific radioactivity. Preparations can be ready for i.v. injection 50 min from the end of radionuclide production.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2541104&dopt=Abstract
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