Drugs online research references
Eur J Pharmacol. 1990 Feb 27;177(3):201-4.
The effect of antidepressants on aversive periaqueductal gray stimulation in rats.
Jenck F, Broekkamp CL, Van Delft AM.
CNS Pharmacology Department, ORGANON International, Oss, The Netherlands.
The selective serotonin (5-HT) uptake inhibitors fluvoxamine and sertraline had anti-aversive effects when administered acutely. Imipramine and clomipramine, which combine noradrenaline (NA) and 5-HT uptake blocking properties, did not have significant effects, whereas the mixed dopamine (DA)/NA uptake blocker nomifensine decreased the thresholds for escape from aversive periaqueductal gray stimulation. These results suggest that indirect 5-HT receptor activation suppresses periaqueductal gray aversion. Conversely, indirect DA and perhaps NA receptor activation appears to enhance periaqueductal gray aversion in rats.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2107091&dopt=Abstract
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Biull Eksp Biol Med. 1990 Dec;110(12):616-7.
[Specifics of participation of dopaminergic and serotoninergic systems of the brain in latent inhibition based on pharmacological models]
[Article in Russian]
Loskutova LV, Luk'ianenko FIa.
Single intraperitoneal injections of haloperidol (0.5 mg/kg) or sertralin (5 mg/kg) or 20 preexpositions of conditional stimulus before conditioning induced similar changes of passive avoidance reactions of rats. The combinative application of drugs (sertralin 1h and bupropion 30 min before conditioning) simultaneously enhancing activity of serotonin and dopamine in brain did not produce changes of passive avoidance reaction comparing with intact control. The results obtained showed that high selective drugs and analysis of latent inhibition of some parameters enable creation of pharmacological models and their use as instrument at experimental study of neurochemical mechanisms of attention.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2128040&dopt=Abstract
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Psychopharmacology (Berl). 1990;100(4):470-6.
[3H] sertraline binding to rat brain membranes.
Koe BK, Lebel LA, Welch WM.
Central Research Division, Pfizer Inc., Groton, CT 06340.
Tritiated sertraline, a radiolabeled form of a potent and selective inhibitor of serotonin uptake, was found to bind with high affinity to rat whole brain membranes. Characterization studies showed that [3H] sertraline binding occurred at a single site with the following parameters: KD 0.57 nM, Bmax 821 fmol/mg protein, nH 1.06. This binding was reversible; the dissociation constant calculated from kinetic measurements (KD 0.81 nM) agreed with that determined by saturation binding experiments. [3H] Sertraline binding in the presence of serotonin, paroxetine, fluoxetine or imipramine suggested competitive inhibition of binding (large increase in KD with little change in Bmax). The rank order of potency of inhibition of [3H] sertraline binding was similar to that of inhibition of serotonin uptake for known uptake inhibitors and the 1-amino-4-phenyltetralin uptake blockers. A marked decrease in ex vivo [3H] sertraline binding in the brain of rats 7 days after treatment with p-chloroamphetamine was consistent with the loss of serotonin uptake sites induced by this agent. The results of our study indicated that [3H] sertraline labels serotonin uptake sites in rat brain.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2138796&dopt=Abstract
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