Drugs online research references
J Neural Transm. 1997;104(1):89-96.
Regional distribution of specific high affinity binding sites for 3H-imipramine and 3H-paroxetine in human brain.
Rosel P, Menchon JM, Oros M, Vallejo J, Cortadellas T, Arranz B, Alvarez P, Navarro MA.
Hormone Unit, Hospital Princeps d'Espanya, Barcelona, Spain.
The binding of 3H-paroxetine and 3H-imipramine has been compared in 17 different regions of 12 human control brains. Our findings reveal that the regional distribution is similar for both radioligands and their bindings tend to be parallel in the brain. The highest binding site density was found in basal ganglia (hypothalamus Bmax 780 +/- 102 fmol/mg protein for 3H-imipramine binding and Bmax 515 approximately 83 for 3H-paroxetine binding). The lowest values were found in cortical areas (cingulate cortex 191 +/- 18.5 fmol/mg for 3H-imipramine binding and 88 +/- 7.5 fmol/mg for 3H-paroxetine binding). The Kd values for 3H-paroxetine binding to neuronal membranes were similar in all brain regions (mean +/- s.d. Kd 0.07 +/- 0.007 nM) and also for 3H-imipramine binding (mean +/- s.d. Kd 1.05 +/- 0.12 nM). As these values are the same as in platelet membrane, the results obtained indicate that both binding sites are identical in neuronal and in platelet membranes. These findings suggest that both ligands are good markers of the 5HT transporter. However, the higher affinity of 3H-paroxetine confirms that this compound is a better radioligand for the 5HT uptake site.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9085196&dopt=Abstract
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Aust N Z J Psychiatry. 1997 Feb;31(1):105-13.
Juvenile obsessive-compulsive disorder.
Wever C, Rey JM.
Rivendell Adolescent Unit, Concord West, New South Wales, Australia.
OBJECTIVE: To describe the characteristics of a series of children and adolescents with obsessive-compulsive disorder (OCD) and evaluate the outcome of treatment. METHOD: Type of symptoms, severity before and after treatment and factors associated with outcome were examined in a large group (n = 82) of consecutive OCD cases referred for treatment. RESULTS: Most children (95%) had both obsessions and compulsions. Symptoms had been present for 2 years on average. Seventy-one per cent (n = 57) of all eligible patients completed a combined behavioural and pharmacological protocol. Among these, there was a 68% remission rate and a 60% decrease of symptoms at 4 weeks. Comorbidity with oppositional defiant disorder and high aggression scores were associated with poor outcome. CONCLUSIONS: Juvenile OCD can be treated effectively in a standard clinical setting. Treatment programs of the kind described are accepted by young people. It remains to be seen whether in this age group a combined treatment produces better results than medication alone or cognitive-behaviour therapy alone.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9088493&dopt=Abstract
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Synapse. 1997 Apr;25(4):345-9.
N-substituted phenyltropanes as in vivo binding ligands for rapid imaging studies of the dopamine transporter.
Scheffel U, Lever JR, Abraham P, Parham KR, Mathews WB, Kopajtic T, Carroll FI, Kuhar MJ.
Division of Nuclear Medicine and Radiation Health Sciences, Johns Hopkins Medical Institutions, Baltimore, Maryland 21205-2179, USA.
Variously substituted phenyltropanes are proven as superb binding ligands for the dopamine transporter (DAT). In this study, we examine four N-substituted phenyltropanes which are derivatives of RTI-55 as in vivo binding ligands in mice. In this series, the methyl group on the nitrogen was replaced by a propyl (RTI-310), an allyl (RTI-311), a butyl (RTI-312), or a fluoropropyl (RTI-313) group. The in vitro binding potencies of these compounds at rat striatal DAT varied somewhat but were about 1 nM. While these compounds did not display marked selectivity for the dopamine transporter, they were more selective than RTI-55. Injection of the radiolabeled compound into mice resulted in striatal-to-cerebellar ratios that varied from about 4.5-6.5. The ratios peaked most rapidly for RTI-311 and RTI-313, at about 20 min. Pharmacological inhibition studies indicated that these compounds were binding to DATs in the striatum, as expected. These findings suggest that some compounds of this type may be excellent in vivo binding ligands for rapid imaging studies of the DAT.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9097393&dopt=Abstract
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