Drugs online research references
Ann Neurol. 1983 Apr;13(4):462-5.
Analgesic activity of tricyclic antidepressants.
Spiegel K, Kalb R, Pasternak GW.
Amitriptyline (median effective dose [ED50] 1.2 mg per kilogram of body weight), imipramine (ED50 2.3 mg/kg), and their demethylated derivatives nortriptyline (ED50 1.9 mg/kg) and desimipramine (ED50 3.2 mg/kg) are active analgesics as indicated by the mouse writhing assay. Although not as potent as morphine (ED50 0.2 mg/kg), the antidepressants were up to 70 times more potent than aspirin (ED50 91 mg/kg). The actions of amitriptyline were not affected by the specific opiate antagonist naloxone but were markedly attenuated in animals whose monoamine levels had been depleted with reserpine. Central mechanisms appear important since amitriptyline (ED50 4.6 micrograms) was potent when administered intracerebroventricularly.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6838179&dopt=Abstract
Brain Res. 1984 Nov 12;321(2):347-51.
The complex binding of tricyclic antidepressants to rat brain: the case of nortriptyline.
Biegon A.
[3H]Nortriptyline (NT) binding to rat brain sections was characterized using saturation and competition experiments, quantitative autoradiographic localization and monoaminergic lesions. [3H]NT binding exhibits a saturable component in the nM range (high affinity binding). Final saturation is reached only in micromolar concentrations (low affinity binding). The high affinity binding sites of [3H]NT appear in areas rich in noradrenergic and serotonergic terminals, and are decreased by 6-OHDA and 5,7-DHT lesions, to an extent depending on the brain region and the relative density of noradrenergic and serotonergic terminals there. We conclude that [3H]NT binds with high affinity to both noradrenergic and serotonergic nerve terminals, and with low affinity to other yet uncharacterized entities. This complex binding pattern is compatible with the multiplicity of biochemical, physiological and behavioral effects of NT and tricyclic antidepressants in general.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6498524&dopt=Abstract
Can J Neurol Sci. 1991 May;18(2):132-6.
The effect of tricyclic antidepressants on cortex- and amygdala-kindled seizures in the rat.
Yacobi R, Burnham WM.
Department of Pharmacology, University of Toronto, Ontario, Canada.
The anticonvulsant effects of amitriptyline, imipramine, nortriptyline and desipramine were tested against focal and generalized seizures, triggered from either the amygdala or the cortex in fully kindled rats. Tests were administered on a 72- or a 24-hour schedule. Significant seizure suppression was achieved with only one drug, amitriptyline, and it occurred only at toxic or near-toxic doses. The differential, low-dose suppression of amygdala-kindled seizures, reported in earlier studies, was not seen in the present experiments. It may occur only in the short-interval test paradigms used by previous experimenters.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1906366&dopt=Abstract
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