Drugs online research references
Br J Pharmacol. 1981 Sep;74(1):81-6.
Use of potentiation of thyrotrophin releasing hormone (TRH)-induced hyperthermia as a test for screening antidepressants which activate alpha-adrenoceptor systems.
Desiles M, Rips R.
1 The minimal dose which significantly potentiates the hyperthermia induced by thyrotrophin releasing hormone (TRH, 40 mg/kg i.p.) in mice has been established for tricyclic and other antidepressants (imipramine, amitriptyline, clomipramine, nortriptyline, maprotiline, nomifensine, viloxazine) including a specific inhibitor of noradrenaline (NA) uptake (nisoxetine). 2 The minimal effective dose in this test has been compared with the minimal dose of the same compounds antagonizing reserpine-induced hypothermia. The ratio of the two doses for each substance indicates that potentiation of TRH-induced hyperthermia is, in general, the more sensitive test. 3 A correlation seems to exist between the alpha-adrenergic effect of antidepressants and the potentiation of TRH- induced hyperthermia. Those antidepressants which do not act on alpha-adrenergic systems (butriptyline, amineptine, trazodone, danitracen, fluoxetine) are inactive in this test. 4 This property may be used to select antidepressants that activate alpha-adrenoceptor systems.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6115696&dopt=Abstract
Ann Otol Rhinol Laryngol. 1989 Nov;98(11):867-72.
Treatment of depressed tinnitus patients with nortriptyline.
Sullivan MD, Dobie RA, Sakai CS, Katon WJ.
Department of Psychiatry and Behavioral Sciences, University of Washington, Seattle.
Patients disabled by tinnitus show a high prevalence of major depression. Furthermore, tinnitus produces patterns of disability similar to those produced by major depression. To explore further this link between tinnitus and depression, and to investigate the efficacy of treating depression in the treatment of tinnitus, a single-blind, placebo-washout, nonrandomized pilot study of the tricyclic antidepressant nortriptyline (hydrochloride) was undertaken in disabled tinnitus patients who also met diagnostic criteria for major depression. Nineteen patients began the study, two responded to placebo, and two dropped out prior to completion. Fourteen considered their tinnitus improved, and 12 chose to continue taking nortriptyline after the study. Depression severity decreased, on the average, by 65% (p less than .0001). Tinnitus loudness measured by audiometric matching decreased by a mean of 10 dB or 50% (p less than .02). Self-reports of tinnitus loudness and severity, somatic and psychologic symptoms, and psychosocial dysfunction all showed significant improvement with treatment. These results suggest that what initially appears to be an irreversible otologic disability in these patients may be in large part a reversible psychiatric disability.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2817678&dopt=Abstract
J Med Chem. 1988 May;31(5):913-9.
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
Hogberg T, Ross SB, Strom P, Grunewald GL, Creese MW, Bunce JD.
Research and Development Laboratories, Astra Alab AB, Sodertalje, Sweden.
A number of tertiary and secondary homoallylic amines, i.e. (Z)- and (E)-4-(4-bromophenyl)-4-(3-pyridyl)-3-buten-1-ylamines, were synthesized in diastereomerically pure forms. The compounds were evaluated as neuronal norepinephrine (NE) and serotonin (5-HT) uptake inhibitors under in vitro and ex vivo conditions and compared with the tricyclics amitriptyline and nortriptyline having homoallylic side chains and with the corresponding diastereomers in the zimeldine series having allylic side chains. The Z isomers of the new homoallylic derivatives (3Z, 4Z) were specific 5-HT uptake inhibitors in analogy with the corresponding allylic derivatives zimeldine (1Z) and norzimeldine (2Z). Likewise, the selectivity profile of the homoallylic (3E, 4E) and the allylic (1E, 2E) derivatives was comparable. In general, the homoallylic compounds were less potent inhibitors than their allylic counterparts. The similarities and discrepancies were evaluated in terms of conformational preferences determined by CAMSEQ molecular mechanics calculations. Homonorzimeldine (4Z) can accommodate energetically favored, but less populated, conformations having amino nitrogen atom to aromatic ring center distances comparable to those in norzimeldine. These facts correlate to retained 5-HT selectivity but diminished potency of 4Z compared to 2Z.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2966246&dopt=Abstract
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