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Chemical Compound Review

Amizyl     2-diethylaminoethyl 2-hydroxy-2,2-diphenyl...

Synonyms: Benactyzin, BENACTYZINE, Benacticina, Benactizina, Benactyzinum, ...
 
 
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Disease relevance of Lucidil

  • In a study aimed toward developing new, selective antimuscarinic drugs with potential utility in the treatment of urinary incontinence associated with bladder muscle instability, a series of N-substituted 5-(aminomethyl)-3,3-diphenyl-2(3H)-furanones, conformationally-constrained lactone relatives of benactyzine, was prepared [1].
  • Benactyzine is used to treat organophosphate poisoning and drofenine acts on smooth muscle to stop muscle spasms [2].
  • Benactyzine-induced mydriasis was also determined for its possible role in photophobic-induced errors [3].
 

Psychiatry related information on Lucidil

 

High impact information on Lucidil

 

Biological context of Lucidil

  • Maximum protection, as determined by a shift of the LD50 for the two OP agents, was observed with the cholinolytic benactyzine [12].
  • Our experiments assess the time course and severity of benactyzine effects on visual acuity for static and moving targets, amplitude and dynamics of accommodation, pupil response to light and the spatial contrast sensitivity function [13].
 

Anatomical context of Lucidil

  • The activity of individual neurons of the visual cortex was recorded simultaneously in behavioral experiments on monkeys before and after the systemic administration of a blocker of M-cholinoreceptors, amizil (0.8-1.0 mg/kg) [14].
  • Aminazine and amizil do not alter the directionality of the influence of the stimulation of the posterior hypothalamus on the responses of the visual cortex; however, they do significantly attenuate the degree of expressivity and the dynamics of this influence [15].
 

Associations of Lucidil with other chemical compounds

  • Both drugs were competitive inhibitors of BChE and the Ki values of benactyzine and drofenine were calculated to be 0.010 +/- 0.001 and 0.003 +/- 0.000 mM, respectively, using the Systat (version 5.03, 1991) nonlinear regression analysis software package [2].
  • When the pretreatment included four components (pyridostigmine, A, M and B), the LD50 of Soman was raised 30.8 times in rabbits [16].
  • Shifts in spatial synchronization of rabbit cortex potentials elicited by application of acetylcholine and amizil to the visual cortex [17].
  • When a small amount of sodium ion was applied to the taenia before or after the treatment with the antispasmodics, the relaxation in response to papaverine was augmented, but those in response to Aspaminol and benactyzine were not affected [18].
 

Analytical, diagnostic and therapeutic context of Lucidil

  • Delayed discrimination of shape, contrast, and size worsened after treatment with amizil at a dose of 0.45-0.50 mg/kg, while decreases in the duration of short-term storage of information relating to color started after amizil doses of 0.6-0.8 mg/kg [6].

References

  1. Synthesis and antimuscarinic properties of some N-substituted 5-(aminomethyl)-3,3-diphenyl-2(3H)-furanones. Kaiser, C., Spagnuolo, C.J., Adams, T.C., Audia, V.H., Dupont, A.C., Hatoum, H., Lowe, V.C., Prosser, J.C., Sturm, B.L., Noronha-Blob, L. J. Med. Chem. (1992) [Pubmed]
  2. Inhibition effects of benactyzine and drofenine on human serum butyrylcholinesterase. Bodur, E., Cokuğraş, A.N., Tezcan, E.F. Arch. Biochem. Biophys. (2001) [Pubmed]
  3. Visual and spatial trials paired in a new behavioral procedure: effects of benactyzine. Grauer, E., Kapon, Y. Pharmacol. Biochem. Behav. (1993) [Pubmed]
  4. Differentiating analgesic and non-analgesic drug activities on rat hot plate: effect of behavioral endpoint. Carter, R.B. Pain (1991) [Pubmed]
  5. Behavioral effects of some diphenyl-substituted antimuscarinics: comparison with cocaine and atropine. Witkin, J.M., Genovese, R.F., Witkin, K.M., Chiang, P.K. Pharmacol. Biochem. Behav. (1992) [Pubmed]
  6. Specific characteristics of cholinergic mechanisms of short-term memory in monkeys for different types of visual information: the effects of amizil. Dudkin, K.N., Chueva, I.V. Neurosci. Behav. Physiol. (1999) [Pubmed]
  7. Molecular modification of anticholinergics as probes for muscarinic receptors. 3. Conformationally restricted analogues of benactyzine. Flavin, M.T., Lu, M.C., Thompson, E.B., Bhargava, H.N. J. Med. Chem. (1987) [Pubmed]
  8. The effects of atropine, benactyzine, and physostigmine on a repeated acquisition baseline in monkeys. Penetar, D.M. Psychopharmacology (Berl.) (1985) [Pubmed]
  9. Influence of trimedoxime bromide on degradation of benactyzine in acidic injectable solutions. Rubnov, S., Amisar, S., Lomnicky, Y., Schneider, H. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. (1999) [Pubmed]
  10. An ethologically based, stimulus and gender-sensitive nonhuman primate model for anxiety. Newman, J.D., Farley, M.J. Prog. Neuropsychopharmacol. Biol. Psychiatry (1995) [Pubmed]
  11. Treatment of intoxication with GV compound in laboratory rats. Fusek, J., Bajgar, J. Sborník vědeckých prací Lékařské fakulty Karlovy university v Hradci Králové. (1994) [Pubmed]
  12. Actions and interactions of cholinolytics and cholinesterase reactivators in the treatment of acute organophosphorus toxicity. Das Gupta, S., Ghosh, A.K., Chowdhri, B.L., Asthana, S.N., Batra, B.S. Drug and chemical toxicology. (1991) [Pubmed]
  13. Effects of benactyzine hydrochloride on dynamic vision functions. Brown, B., Haegerstrom-Portnoy, G., Baker, R., Adams, A.J., Jones, R.T. Aviation, space, and environmental medicine. (1982) [Pubmed]
  14. Processes of visual recognition in monkeys and their neuronal correlates in the visual cortex: the influence of a blocker of M-cholinoreceptors. Dudkin, K.N., Kruchinin, V.K., Chueva, I.V. Neurosci. Behav. Physiol. (1994) [Pubmed]
  15. Influence of the posterior hypothalamus on the visual cortex in various states of the reticular formation. Gadzhieva, N.A., Dzhavadov, D.G., Rzaeva, N.M. Neurosci. Behav. Physiol. (1991) [Pubmed]
  16. Effects of carbamates on whole blood cholinesterase activity: chemical protection against soman. Heyl, W.C., Harris, L.W., Stitcher, D.L. Drug and chemical toxicology. (1980) [Pubmed]
  17. Shifts in spatial synchronization of rabbit cortex potentials elicited by application of acetylcholine and amizil to the visual cortex. Kurova, N.S., Yastrebtsov, A.I., Murav'ev, I.V. Neurosci. Behav. Physiol. (1988) [Pubmed]
  18. Mechanism of relaxant action of papaverine. III. Comparison of sodium ion dependencies on the relaxant effects of papaverine, Aspaminol and benactyzine in guinea-pig taenia coli. Sunagane, N., Sakata, T., Uruno, T., Kubota, K. J. Pharmacobio-dyn. (1983) [Pubmed]
 
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