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. 1979 Sep;67(1):115–122.

Production of catalepsy and depletion of brain monoamines by a butyrophenone derivative.

L D Fuenmayor, M Vogt
PMCID: PMC2043615  PMID: 574039

Abstract

1 The cataleptic and monoamine-depleting effects of a butyrophenone derivative (4'-fluoro-4-[[4-(p-fluorophenyl)-3-cyclohexen-1-yl]-amino]-butyrophenone hydrochloride, U-32, 802A) were studied in rats and mice and compared with those of tetrabenazine. 2 Catalepsy was evaluated by means of a modified grid test which allowed the repetition of the test in the same animal several times without affecting the results. Both drugs produced a dose-related cataleptic state of similar time course. 3 Like tetrabenazine, U-32, 802A induced a large reduction in the content of 5-hydroxytryptamine, dopamine and noradrenaline in different parts of the brain, with a concomitant elevation in the metabolites 5-hydroxyindol-3-yl acetic acid and homovanillic acid. The time courses of the catalepsy and the reduction in brain monoamines were very similar. 4 The activity of U-32, 802A suggested that the drug, although chemically a butyrophenone, might act primarily at the presynaptic organelle for storage of monoamines in a way similar to tetrabenazine.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Ahtee L., Sharman D. F., Vogt M. Acid metabolites of monoamines in avian brain; effects of probenecid and reserpine. Br J Pharmacol. 1970 Jan;38(1):72–85. doi: 10.1111/j.1476-5381.1970.tb10337.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. CARLSSON A., LINDQVIST M. EFFECT OF CHLORPROMAZINE OR HALOPERIDOL ON FORMATION OF 3METHOXYTYRAMINE AND NORMETANEPHRINE IN MOUSE BRAIN. Acta Pharmacol Toxicol (Copenh) 1963;20:140–144. doi: 10.1111/j.1600-0773.1963.tb01730.x. [DOI] [PubMed] [Google Scholar]
  3. COSTA E., GESSA G. L., BRODIE B. B. Influence of hypothermia on chlorpromazine-induced changes in brain amine levels. Life Sci. 1962 Jul;1:315–319. doi: 10.1016/0024-3205(62)90125-x. [DOI] [PubMed] [Google Scholar]
  4. Costall B., Hui S. C., Naylor R. J. Correlation between multitest and single test catalepsy assessment. Neuropharmacology. 1978 Sep;17(9):761–764. doi: 10.1016/0028-3908(78)90090-4. [DOI] [PubMed] [Google Scholar]
  5. Gerardy J., Cajgfinger G. Action de trois neuroleptiques sur le taux de DOPAC dans le noyau caudé du rat. Arch Int Pharmacodyn Ther. 1972 Sep;199(1):197–200. [PubMed] [Google Scholar]
  6. LAVERTY R., SHARMAN D. F. MODIFICATION BY DRUGS OF THE METABOLISM OF 3,4-DIHYDROXYPHENYLETHYLAMINE, NORADRENALINE AND 5-HYDROXYTRYPTAMINE IN THE BRAIN. Br J Pharmacol Chemother. 1965 Jun;24:759–772. doi: 10.1111/j.1476-5381.1965.tb01632.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Lahti R. A., Lednicer D. Effect of a butyrophenone derivative, U-32,802A, on brain biogenic amines. Biochem Pharmacol. 1974 Jun 15;23(12):1701–1705. doi: 10.1016/0006-2952(74)90397-9. [DOI] [PubMed] [Google Scholar]
  8. Murphy G. F., Robinson D., Sharman D. F. The effect of tropolone on the formation of 3,4-dihydroxyphenylacetic acid and 4-hydroxy-3-methoxyphenylacetic acid in the brain of the mouse. Br J Pharmacol. 1969 May;36(1):107–115. doi: 10.1111/j.1476-5381.1969.tb08308.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. PLETSCHER A. Release of 5-hydroxytryptamine by benzoquinolizine derivatives with sedative action. Science. 1957 Sep 13;126(3272):507–507. doi: 10.1126/science.126.3272.507. [DOI] [PubMed] [Google Scholar]
  10. Pletscher A. Effect of neuroleptics and other drugs on monoamine uptake by membranes of adrenal chromaffin granules. Br J Pharmacol. 1977 Mar;59(3):419–424. doi: 10.1111/j.1476-5381.1977.tb08395.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Roffler-Tarlov S., Sharman D. F., Tegerdine P. 3,4-dihydroxyphenylacetic acid and 4-hydroxy-3-methoxyphenylacetic acid in the mouse striatum: a reflection of intra- and extra-neuronal metabolism of dopamine? Br J Pharmacol. 1971 Jul;42(3):343–351. doi: 10.1111/j.1476-5381.1971.tb07118.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Saner A., Pletscher A. A benzo[a]quinolizine derivative with a neuroleptic-like action on cerebral monoamine turnover. J Pharmacol Exp Ther. 1977 Dec;203(3):556–563. [PubMed] [Google Scholar]
  13. Sharman D. F. Changes in the metabolism of 3,4-dihydroxyphenylethylamine (dopamine) in the striatum of the mouse induced by drugs. Br J Pharmacol Chemother. 1966 Nov;28(2):153–163. doi: 10.1111/j.1476-5381.1966.tb01881.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Simon P., Malatray J., Boissier J. R. Antagonism by amantadine of prochlorpemazine-induced catalepsy. J Pharm Pharmacol. 1970 Jul;22(7):546–547. doi: 10.1111/j.2042-7158.1970.tb10567.x. [DOI] [PubMed] [Google Scholar]
  15. Stanley M. E., Glick S. D. Interaction of drug effects with testing procedures in the measurement of catalepsy. Neuropharmacology. 1976 Jul;15(7):393–394. doi: 10.1016/0028-3908(76)90115-5. [DOI] [PubMed] [Google Scholar]
  16. TEDESCHI D. H., TEDESCHI R. E., COOK L., MATTIS P. A., FELLOWS E. J. The neuropharmacology of trifluoperazine: a potent psychotherapeutic agent. Arch Int Pharmacodyn Ther. 1959 Oct 1;122:129–143. [PubMed] [Google Scholar]

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