Drugs online research references









J Pharm Pharmacol. 1987 May;39(5):392-4.
The inhibition of monoamine oxidase by tricyclic antidepressants: the influence of the nature of the substrate and the source of the enzyme.

Green AL, McGachy HA.

Five tricyclic antidepressants, amitriptyline, clomipramine, desipramine, imipramine and iprindole, have comparable potencies as inhibitors of monoamine oxidase in rodent brain and liver. With rodent brain, potency was always greater with phenethylamine as substrate than with benzylamine, and was generally least with 5-HT. With mouse liver, in which monoamine oxidase is mainly B type, potency with tyramine and dopamine as substrates was close to that found with phenethylamine. The kinetics of inhibition varied with both the substrate and the tissue, and were inconsistent with a simple ping-pong model for substrate oxidation. The relevance of these observations to clinical effectiveness is discussed.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2886590&dopt=Abstract




Nippon Yakurigaku Zasshi. 1987 Apr;89(4):175-80.
[Specific inhibitory action of a novel antidepressant paroxetine on 5-HT uptake]

[Article in Japanese]

Tanigaki N, Manno K, Sugihara K, Miki N, Ichida S, Yoshida H.

Effect of a novel antidepressant, paroxetine, on the uptake of serotonin (5-HT), noradrenaline (NA) and dopamine (DA) as well as on various neuro-receptors were investigated in comparison with those of the tricyclic antidepressants amitriptyline, chlorimipramine and imipramine. Paroxetine showed a potent 5-HT uptake inhibitory action, giving the NA/5-HT ratio of 886 in comparison with the ratios of 1.7, 15 and 1.5 for amitriptyline, chlorimipramine and imipramine, respectively. On the other hand, paroxetine showed almost no inhibitory action on the binding of the [3H]-labeled ligands examined in this study [( 3H]quinuclidinyl benzilate, [3H]5-HT, [3H]ketanserine, [3H]pyrilamine, [3H]dihydroalprenolol, [3H]prazosin, [3H]clonidine and [3H]spiroperidol). In contrast, the tricyclic antidepressants showed inhibitory action on a number of bindings and also revealed comparatively high affinities especially for muscarine, histamine-1 and alpha 1-adrenaline receptors responsible for the side effects. From the above findings, it can be concluded that paroxetine has only a weak affinity for various neuro-receptors and inhibits specifically 5-HT uptake.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3038714&dopt=Abstract




Brain Res. 1988 Aug 9;457(2):281-6.
The effect of amitriptyline on growth of olfactory and cerebral neurons in vitro.

Farbman AI, Gonzales F, Chuah MI.

Department of Neurobiology and Physiology, Northwestern University, Evanston, IL 60208.

The tricyclic antidepressant drug amitriptyline has a detrimental effect on neurite outgrowth in primary explant cultures containing either olfactory receptor neurons or cerebral neurons, from both rat and chick embryos. When the drug is added to the culture medium in doses similar to the plasma concentrations known to be therapeutic in humans, the number of explant cultures expressing neurites is significantly reduced. In higher doses, amitriptyline reduces the amount of olfactory marker protein synthesized by organ cultures of olfactory mucosa.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3219556&dopt=Abstract













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