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Tri cyclic anti depressants as anti muscarinic drugs in vivo and in vitro studies


, : Tri cyclic anti depressants as anti muscarinic drugs in vivo and in vitro studies. Biochemical Pharmacology 26(17): 1559-1568

Antagonistic activity of nortriptyline, amitriptyline and imipramine to the hypothermic and tremorigenic activity of oxotremorine was determined in mice. The peripheral anticholinergic relative potencies of these drugs were evaluated by following dose-dependent time profiles of their mydriatic activity. Binding constants of the antidepressant agent toward the central muscarinic receptor from the mouse whole brain homogenate were determined in vitro and could be correlated with ED50 values found for the 3 drugs' in vivo responses. The 3 antidepressants tested were found to be 100-fold less active than scopolamine.cntdot.HBr in all 4 biological preparations selected. Their anticholinesterase activity towards the enzyme in whole mouse brain homogenate apparently was too low to make any possible contribution to their activity in vivo. Relationships between structure and function and the possible contribution of their antimuscarinic property to the observed in vivo effects are discussed.

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Accession: 006839947

PMID: 901576

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Other references

Grubner, O.; First, M.W.; Huber, G.L., 1980: Gas chromatographic determination of nicotine in gases and liquids with suppression of adsorption effects. Prior reports have indicated that analysis of nicotine to study the effects of tobacco smoking at pg/ml levels was unreliable. Significant and variable nicotine adsorption on the different materials used during analysis was recognized as a source...

Ciccarelli, O.; Toosy, A.T.; Hickman, S.J.; Parker, G.J.M.; Wheeler-Kingshott, C.A.M.; Miller, D.H.; Thompson, A.J., 2005: Optic radiation changes after optic neuritis detected by tractography-based group mapping. Postmortem data suggest that trans-synaptic degeneration occurs in the lateral geniculate nucleus after optic nerve injury. This study investigated in vivo the optic radiations in patients affected by optic neuritis using fast marching tractograph...

Yang, K.; Yu, M., 1994: Evidence for distinct isoforms of 11 beta-hydroxysteroid dehydrogenase in the ovine liver and kidney. We have previously identified a unique 11 beta-hydroxysteroid dehydrogenase (11 beta-HSD) transcript in the ovine kidney. To examine whether this is indicative of a distinct isoform with respect to enzymatic activity, we studied and compared the c...

Perepelkin, V.S.; Varaksin, V.S.; Zhuravlev, G.P., 1980: Experience in conducting spot checks of project documentation. Voenno-Meditsinskii Zhurnal (): 47-50

Rice J.M.; London W.T.; Palmer A.E.; Sly D.L.; Williams G.M., 1977: Direct and trans placental carcinogenesis by ethylnitroso urea in the patas monkey erythrocebus patas. Proceedings of the American Association for Cancer Research 18: 53

Lancastre, F.; Vianey-Liaud, M.; Coutris, G.; Bolognini-Treney, J.; Mougeot, G.; Ouaghlissi, JP., 1989: Resistance a la dessiccation de Biomphalaria glabrata adultes infestes par plusieurs miracidiums de Schistosoma mansoni. 1200 adult Biomphalaria glabrata were submitted during 6 weeks to anhydrobiosis condition. Some snails were healthy, some were previously infected 3 days or 12 days ago with 8 .+-. 2 miracidia of Schistosoma mansoni, others were shedding cercariae...

Minota, S.; Jarjour, W.N.; Roubey, R.A.; Mimura, T.; Winfield, J.B., 1990: Reactivity of autoantibodies and DNA/anti-DNA complexes with a novel 110-kilodalton phosphoprotein in systemic lupus erythematosus and other diseases. Utilizing nonionic detergent lysates of human lymphoid and non-lymphoid cells as substrate, IgM and/or IgG antibodies to a 110-kDa/isoelectric point 5.4 phosphoprotein (110K) was demonstrated in serum from patients with SLE or certain other system...

Wu, M.; Gordon, R.E.; Herbert, R.; Padilla, M.; Moline, J.; Mendelson, D.; Litle, V.; Travis, W.D.; Gil, J., 2010: Case report: Lung disease in World Trade Center responders exposed to dust and smoke: carbon nanotubes found in the lungs of World Trade Center patients and dust samples. Environmental Health Perspectives 118(4): 499-504

Stein, V.; Hoerner, K., 1990: The abduction orthesis variant in treatment of perthes' disease. The abduction orthesis presents a new variant in our treatment of Perthes' disease. The containment was obtained conservatively using this splint. This orthesis was tolerated very well by all children.

Santosa, Frans; Moysidis, Theodoros; Assenheimer, Bernd; Bültemann, Anke; Kröger, Knut, 2012: Role of lymphatic massage in Germany. Lymphoedema is an important cause of morbidity in the population, but little is known of its epidemiology and impact on patients or health services. Thus we looked for use of manual lymphatic drainage (MLD) in Germany with its unique health system...