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Chemical Compound Review

DEXETIMIDE     (3R)-3-(1-benzyl-4- piperidyl)-3-phenyl...

Synonyms: Dexetimida, Levetimide, Dexetimidum, l-Benzetimide, SureCN1651291, ...
 
 
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Disease relevance of Tremblex

 

Psychiatry related information on Tremblex

 

High impact information on Tremblex

  • Here we describe the solubilization of muscarinic acetylcholine receptors with digitonin and their purification by affinity chromatography using an affinity gel which consisted of dexetimide coupled to Affi-Gel 10 (i.e., carboxy N-hydroxysuccinimide esters linked via a 1 nm spacer arm to agarose beads) [7].
  • Binding competition curves with the antagonists atropine, dexetimide, and NMS gave KD values of 3.5, 3.5, and 0.5 nM, respectively [8].
  • The effects of dexetimide, levetimide, 4-diphenylacetoxy-N-ethylpiperidine ethobromide, AF-DX 116, and telenzepine on N-[3H]methylscopolamine binding were not affected or were barely affected by d-tubocurarine; these compounds preferentially recognize another binding site (probably the muscarinic binding site) [9].
  • These results demonstrate that a combination of the distinct kinetics of dexetimide and NMS and the receptor subtype selectivity of guanylpirenzepine and AF-DX 116 provides a valuable labeling strategy to examine the distribution and localization of the M4 (m4) muscarinic receptor subtype in brain, peripheral tissues, and cell lines [10].
  • In vitro, the drug had no effect on striatal choline acetyltransferase activity up to a concentration of 160 microM and only weakly displaced (3H) dexetimide from its specific muscarinic receptor binding sites in striatum (IC50, 2 X 10(-4) M) [11].
 

Chemical compound and disease context of Tremblex

 

Biological context of Tremblex

 

Anatomical context of Tremblex

 

Associations of Tremblex with other chemical compounds

  • The selective M1-antagonist pirenzepine, the mixed M1/M2-antagonist dexetimide and the cardioselective M2-antagonist gallamine were used as tools for identification of the receptors [20].
 

Analytical, diagnostic and therapeutic context of Tremblex

References

  1. Central cardiovascular effects of physostigmine in the cat; possible cholinergic aspects of blood pressure regulation. de Wildt, D.J., Porsius, A.J. Archives internationales de pharmacodynamie et de thérapie. (1981) [Pubmed]
  2. Treatment of Parkinsonian syndrome with dexetimide. Deze, J., Völler, G.W. Acta psychiatrica Belgica. (1979) [Pubmed]
  3. Myasthenia gravis: control of drug-induced cholinergic symptoms with dexetimide. Szobor, A. Therapia Hungarica (English edition) (1985) [Pubmed]
  4. Safety and efficacy of prolonged treatment with Tremblex (dexetimide), an antiparkinsonian agent. A controlled study. Zwanikken, G.J., Oei, T.T., Kimya, S., Amery, W. Acta psychiatrica Belgica. (1976) [Pubmed]
  5. Differential effects produced by an anticholinergic on the neuroleptic inhibition of motor behaviour and self-stimulation of the prefrontal cortex in the rat. Mora, F., Alba, F., Sanguinetti, A.M., Rodriguez, J.M., Vives, F. Brain Res. Bull. (1980) [Pubmed]
  6. Episodic barrel rotations induced by intrastriatal injection of quinolinic acid in rats. Inhibition by anticonvulsants. Marrannes, R., Wauquier, A. Pharmacol. Biochem. Behav. (1988) [Pubmed]
  7. Purification of muscarinic acetylcholine receptors by affinity chromatography. André, C., De Backer, J.P., Guillet, J.C., Vanderheyden, P., Vauquelin, G., Strosberg, A.D. EMBO J. (1983) [Pubmed]
  8. Characterization of muscarinic cholinergic receptors on rat pancreatic acini by N-[3H]methylscopolamine binding. Their relationship with calcium 45 efflux and amylase secretion. Dehaye, J.P., Winand, J., Poloczek, P., Christophe, J. J. Biol. Chem. (1984) [Pubmed]
  9. Identification of drugs competing with d-tubocurarine for an allosteric site on cardiac muscarinic receptors. Waelbroeck, M. Mol. Pharmacol. (1994) [Pubmed]
  10. Selective labeling and localization of the M4 (m4) muscarinic receptor subtype. Ferrari-Dileo, G., Waelbroeck, M., Mash, D.C., Flynn, D.D. Mol. Pharmacol. (1994) [Pubmed]
  11. Neurochemical effects of minaprine, a novel psychotropic drug, on the central cholinergic system of the rat. Garattini, S., Forloni, G.L., Tirelli, S., Ladinsky, H., Consolo, S. Psychopharmacology (Berl.) (1984) [Pubmed]
  12. The effects of dexetimide on pimozide-, haloperidol- and pipamperone-induced inhibition of brain self-stimulation in rats. Wauquier, A., Niemegeers, C.J. Archives internationales de pharmacodynamie et de thérapie. (1975) [Pubmed]
  13. Stereoselective binding in cardiac tissue of the enatiomers of benzetimide, and antimuscarinic drug. Gray, J.A., Lüllmann, H., Mitchelson, F., Reil, G.H. Br. J. Pharmacol. (1976) [Pubmed]
  14. Inhibition of efferent sympathetic nerve activity by centrally administered paraoxon in the cat. De Neef, J.H., Borgdorff, P., Porsius, A.J. Eur. J. Pharmacol. (1982) [Pubmed]
  15. The experimental infection of pigs with Campylobacter sputorum subspecies mucosalis. Weaned pigs, with special reference to pharmacologically mediated hypomotility. Roberts, L., Lawson, G.H., Rowland, A.C. Res. Vet. Sci. (1980) [Pubmed]
  16. Central effects of paraoxon on haemodynamics in the cat. de Neef, J.H., Porsius, A.J. Naunyn Schmiedebergs Arch. Pharmacol. (1981) [Pubmed]
  17. Restoration of self-stimulation inhibited by neuroleptics. Wauquier, A., Niemegeers, C.J. Eur. J. Pharmacol. (1976) [Pubmed]
  18. Modulation of the hippocampal alpha-adrenoceptor population by lesion of the serotonergic raphe-hippocampal pathway in rats. Consolo, S., Ladinsky, H., Forloni, G.L., Grombi, P. Life Sci. (1982) [Pubmed]
  19. Comparison of atropine and dexetimide in treatment of intoxications by selected organophosphates. Lüllmann, H., Schmaus, H., Staemmler, C., Ziegler, A. Acta pharmacologica et toxicologica. (1982) [Pubmed]
  20. Subclassification of muscarinic receptors in the heart, urinary bladder and sympathetic ganglia in the pithed rat. Selectivity of some classical agonists. van Charldorp, K.J., de Jonge, A., Thoolen, M.J., van Zwieten, P.A. Naunyn Schmiedebergs Arch. Pharmacol. (1985) [Pubmed]
  21. In vivo biodistribution of two [18F]-labelled muscarinic cholinergic receptor ligands: 2-[18F]- and 4-[18F]-fluorodexetimide. Wilson, A.A., Scheffel, U.A., Dannals, R.F., Stathis, M., Ravert, H.T., Wagner, H.N. Life Sci. (1991) [Pubmed]
 
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