Animal model of depression: tests of three structurally and pharmacologically novel antidepressant compounds. Effects of dopamine uptake inhibitors on schedule-controlled behavior in the squirrel monkey. Rate of binding of various inhibitors at the dopamine transporter in vivo. Rx drugs

Drugs online research references

Pharmacol Biochem Behav. 1982 Jun;16(6):973-7.
Animal model of depression: tests of three structurally and pharmacologically novel antidepressant compounds.

Katz RJ, Sibel M.

Previous studies have identified behavioral and neuroendocrine abnormalities in chronically stressed rats which resemble some of the more prominent features of clinical depression. These abnormalities have proved responsive to pharmacotherapy by standard antidepressant drugs and related somatic treatments. Several structurally and pharmacologically atypical compounds, resembling neither standard agents, nor each other, have recently been identified as clinically effective antidepressants. There drugs do not show typical preclinical response profiles in other drug screening tests and, therefore, represent critical instances for evaluating the selectivity of the chronic stress model. Three drugs were tested, these being iprindole, bupropion, and mianserine; a tricyclic indole, propriophenone, and tetracyclic compound respectively. Four circulating measures, which previously proved most useful in discriminating antidepressant potential, and a measure of circulating corticosterone were obtained for subjects examined factorially in a 2x2x2 experimental design (chronic stress vs none, acute stress vs none, and drugs vs control). All compounds proved capable of reversing chronic stress induced behavioral deficits, and all but one compound reversed the attendant basal hypersecretion of corticosterone. These findings argue that the chronic stress model provides an accurate and selective assessment of the therapeutic potential of both standard and structurally novel compounds.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6810386&dopt=Abstract

word match zyban online literature

Psychopharmacology (Berl). 1982;78(4):377-9.
Effects of dopamine uptake inhibitors on schedule-controlled behavior in the squirrel monkey.

McKearney JW.

Squirrel monkeys responded under a multiple fixed-interval (FI) fixed-ratio (FR) schedule of stimulus-shock termination. Benztropine mesylate (0.03-1.7 mg/kg), bupropion HCl (0.3-5.6 mg/kg), mazindol (0.01-0.3 mg/kg), and nomifensine maleate (0.1-1.0 mg/kg) markedly increased responding under the FI schedule, but not under the FR schedule. Mazindol was about three-times more potent than nomifensine and ten-times more potent than bupropion. Benztropine and mazindol were about equal in potency. The order and relative magnitude of potency differences for mazindol, nomifensine, and bupropion are similar to those reported by others for in vitro inhibition of dopamine uptake in rat striatum, but the relative potency of benztropine was greater in these behavioral experiments than expected from its potency in inhibiting dopamine uptake.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6818602&dopt=Abstract

word match zyban online literature

Psychopharmacology (Berl). 1995 Jun;119(4):376-84.
Rate of binding of various inhibitors at the dopamine transporter in vivo.

Stathis M, Scheffel U, Lever SZ, Boja JW, Carroll FI, Kuhar MJ.

Johns Hopkins University School of Medicine, Department of Radiology, Baltimore, MD 21205, USA.

The rate of entry of drugs into brain is thought to be a factor in their abuse liability. In this investigation, we have examined the rate of entry and binding at dopamine transporters in mouse striatum for a variety of dopamine transporter inhibitors. The method utilized was based on measuring the displacement of 3H-WIN 35,428 from striatal dopamine transporter sites in vivo at different times. Eleven cocaine analogs (RTI-31, RTI-32, RTI-51, RTI-55, RTI-113, RTI-114, RTI-117, RTI-120, RTI-121, WIN 35,065-2, and WIN 35,428) as well as other dopamine uptake site blockers (bupropion, nomifensine, and methylphenidate) were compared with (-) cocaine for their rates of displacement of 3H-WIN 35,428 binding in vivo. The drugs that displayed the fastest occupancy rates were bupropion, (-) cocaine, nomifensine, and methylphenidate. RTI-51, RTI-121, RTI-114, RTI-117, RTI-120, RTI-32, RTI-55, and RTI-113, showed intermediate rates, whereas RTI-31, WIN 35,065-2, and WIN 35,428 exhibited the slowest rates of displacement. While many of the cocaine analogs have proven to be behaviorally and pharmacologically more potent than (-) cocaine, their rates of entry and binding site occupancy were slower than that for (-) cocaine. Earliest times of transporter occupancy by the different drugs were correlated (although weakly) with their degree of lipophilicity (r = 0.59; P < 0.02). Kinetic effects and metabolism of the compounds could complicate the interpretations of these data.(ABSTRACT TRUNCATED AT 250 WORDS)

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7480516&dopt=Abstract

word match zyban online literature

Herbs and Pharmaceuticals Online || Hair Million herbal formula for hair loss and hair growth || Antibiotics and prescription medications online literature ||