Drugs online research references
Eur J Pharmacol. 1987 Sep 11;141(2):187-94.
Sertraline, a selective inhibitor of serotonin uptake, induces subsensitivity of beta-adrenoceptor system of rat brain.
Koe BK, Koch SW, Lebel LA, Minor KW, Page MG.
Department of Pharmacology, Pfizer Inc., Groton, CT 06340.
Subacute administration (b.i.d. for 4 days) of sertraline, a potent and selective inhibitor of serotonin uptake, was found to reduce cyclic AMP generation by the norepinephrine receptor-coupled adenylate cyclase in rat limbic forebrain slices and decrease the number of beta-adrenoceptors in rat cerebral cortex without affecting the affinity of [3H]dihydroalprenolol binding. Co-administration of sertraline and the serotonin agonist, quipazine, at doses at which neither agent had an effect, resulted in desensitization of norepinephrine receptor-coupled adenylate cyclase and down-regulation of beta-adrenoceptors. These findings suggest that increased serotonergic activity may be involved in the induction of subsensitivity of the beta-adrenoceptor system of rat brain by sertraline.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2824215&dopt=Abstract
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Brain Res. 1987 Sep 22;421(1-2):377-81.
Chronic administration of sertraline, a selective serotonin uptake inhibitor, decreased the density of beta-adrenergic receptors in rat frontoparietal cortex.
Byerley WF, McConnell EJ, McCabe RT, Dawson TM, Grosser BI, Wamsley JK.
Department of Psychiatry, University of Utah Medical Center, Salt Lake City 84132.
Sertraline, a potent and selective inhibitor of serotonin uptake, was chronically administered to laboratory rats. Using in vitro receptor autoradiographic techniques, we found that the binding of [3H]dihydroalprenolol ([3H]DHA) was reduced in cortex layers IV-VI. Results of a saturation experiment indicated that the reduction in cortex layer IV was due to a change in number but not affinity of beta-adrenergic receptors.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2825912&dopt=Abstract
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Brain Res. 1988 Jun 28;454(1-2):78-88.
Quantitative autoradiography of serotonin uptake sites in rat brain using [3H]cyanoimipramine.
Kovachich GB, Aronson CE, Brunswick DJ, Frazer A.
Neuropsychopharmacology Unit, Veterans Administration Medical Center, Philadelphia, PA 19104.
The binding of [3H]cyanoimipramine to serotonin uptake sites in rat brain slices was studied using quantitative autoradiography. Binding was of high affinity and was to a single class of binding site. This is in contrast to results previously obtained by others with [3H]imipramine where two binding sites were observed. The sites labeled by [3H]cyanoimipramine had properties consistent with this ligand labeling serotonin uptake sites, as: (1) binding is displaced by drugs which are potent inhibitors of serotonin uptake but not by drugs which are weak inhibitors of uptake; (2) binding is dependent on the presence of sodium ions as is the uptake of serotonin; (3) binding is almost completely eliminated in the brains of rats lesioned by the serotonin neurotoxin 5,7-dihydroxytryptamine; (4) the distribution of binding sites throughout the rat brain is highly correlated with that found previously for [3H]indalpine, a potent serotonin uptake inhibitor, and for [3H]imipramine. The properties of binding of [3H]cyanoimipramine make it an ideal ligand for the quantitative autoradiography of serotonin uptake sites.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2970277&dopt=Abstract
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