Drugs online research references
Nucl Med Biol. 1997 Apr;24(3):251-4.
Radiosynthesis and PET imaging of [N-methyl-11C]LY257327 as a tracer for 5-HT transporters.
Zea-Ponce Y, Baldwin RM, Stratton MD, al-Tikriti M, Soufer R, Schaus JM, Innis RB.
Department of Psychiatry, Yale University School of Medicine, West Haven, CT, USA.
No-carrier-added [N-methyl-11C]LY257327 was synthesized by methylation of the free base of the desmethyl precursor LY214281 with [11C]methyl iodide in anhydrous acetonitrile. Synthesis time was 52 +/- 3 min, radiochemical yield (based on [11C]methyl iodide) was 35 +/- 8%, radiochemical purity was 99 +/- 1%, and specific activity at EOB was 3900 +/- 1300 mCi/mumol. Two in vivo studies in baboon were carried out before and after pretreatment with the selective serotonin reuptake inhibitor citalopram. The first experiment showed high accumulation of radioactivity in midbrain, striatum, and thalamus, with slightly lower accumulation in the occipital and cerebellum regions. The radioactivity concentration peaked 5 min postinjection, decreasing steadily for the rest of the scanning time. The second experiment (blocked with citalopram) showed only partial inhibition of incorporation in all of the same brain regions. Although [N-methyl-11C]LY257327 displayed high brain uptake (5% of injected dose at 5 min postinjection) and localized in serotonergic areas of the brain, its target-to-nontarget ratio and its insensitivity to citalopram blocking suggest that its accumulation is dominated by nonspecific uptake. Therefore, [N-methyl-11C]LY257327 is not a useful agent for measuring serotonin reuptake sites in vivo by positron emission tomography.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9228659&dopt=Abstract
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Br J Psychiatry. 1997 Mar;170:257-63.
Cost-effectiveness of antidepressant treatment reassessed.
Woods SW, Rizzo JA.
Department of Psychiatry, Yale University School of Medicine, CT 06519, USA.
BACKGROUND: A recent simulation concluded that the serotonin-specific reuptake inhibitor (SSRI) paroxetine was more cost-effective than the tricyclic antidepressant (TCA) imipramine, despite substantially higher medication acquisition costs. METHOD: We replicated the previous model and revised key assumptions which drove the results. The revised model was subjected to sensitivity analysis. RESULTS: Most scenarios in the revised model showed that the TCA is equally or more cost-effective than the SSRI. Model revision producing these results were changes in assumptions about switched treatment success rates, treatment length and initial treatment success. The revised model appears sensitive to drug acquisition and delivery costs and costs of treatment failure. CONCLUSIONS: Based on the model, a policy of using TCAs as first-choice antidepressant treatment, with SSRIs reserved for those patients not doing well initially, appears more cost-effective than the reverse sequence. Given limitations in current knowledge about key parameters to include in a simulation model, large prospective random-assignment cost-effectiveness studies are needed.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9229033&dopt=Abstract
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Nucl Med Biol. 1994 Nov;21(8):1083-91.
Highly potent indanamine serotonin uptake blockers as radiotracers for imaging serotonin uptake sites.
Suehiro M, Scheffel UA, Ravert HT, Ricaurte GA, Hatzidimitriou G, Dannals RF, Bogeso KP, Wagner HN Jr.
Division of Nuclear Medicine, Johns Hopkins Medical Institutions, Baltimore, MD 21205, USA.
Two highly potent indanamine serotonin (5-HT) uptake blockers, trans-3'-(4'-bromophenyl)-1-indanamine (trans-[11C]DBPI or [11C]Lu 19-056) and its iodo analog, trans-3'(4'-[125I]iodophenyl)-1-indanamine (trans-[125I]DIPI) were evaluated as radiotracers for imaging 5-HT uptake sites in vivo Trans-[11C]DBPI was synthesized by N-methylation of the normethyl precursor with [11C]iodomethane. Trans-[125I]DIPI was synthesized by iododestannylation of the tributyltin precursor with [125I]NaI. Radiochemical yields for the [11C] and [125I] radiotracers were 34 and 40% with specific activities of 4000 and 1800 mCi/mumol, respectively. In vitro, the iodo analog, trans-DIPI, showed an IC50 value of 0.26 nM in inhibition of [3H]paroxetine binding to 5-HT uptake sites in rat cortex. The potency was found to be equivalent to that of paroxetine or McN5652. In vivo, after i.v. injection into mice, both radiotracers showed high uptake in brain (3-4% dose/whole brain at 15 min) and high accumulation into target tissues such as hypothalamus and olfactory tubercles (7-8% dose/g at 60 min). The binding was blocked by pre-injection of 5 mg/kg of peroxetine. While the in vivo distribution agreed with previously reported 5-HT uptake site distribution, the radiotracers showed high uptake in non-target tissues such as cerebellum, resulting in low target-to-non-target ratios (1.5-1.6 at 60 min). Since washout from non-target regions was slower than from target regions, longer-time observation with 125I up to 6 h did not improve the ratios. HPLC analyses of mouse brain homogenates and blocking studies indicated that the high uptake in non-target regions is not the result of metabolism or any interaction of the radiotracers with those tissues via specific binding sites. In spite of low target-to-non-target ratios, target regions with high density of 5-HT uptake sites, such as the raphe nuclei, superior colliculi and substantia nigra, were visualized with trans-[125I]DIPI by ex vivo autoradiography, since the radiotracer showed high specific binding (total mimus nonspecific binding).
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9234366&dopt=Abstract
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