Lack of postulated opiate-receptor antagonistic properties of compound 48/80

Piotr Janicki, A. Cztonkowski, J. Libich, S. W. Gumutka

Research output: Contribution to journalArticle

Abstract

The previously suggested opiate-receptor antagonistic properties of compound 48/80 were checked both in vivo and in vitro. In electrically stimulated guinea pig ileum and rat vas deferens preparations compound 48/80 did not reverse the inhibition of the twitches caused either by morphine or Met5-enkephalin. In mice hot-plate test compound 48/80 did not decrease the analgesic activity of morphine. In radioreceptor studies compound 48/80 shows rather low affinity to the 3H-naloxone receptor sites from striatal homogenates of the rat, as compared to non-labelled naloxone and on the other hand it produced moderate, as compared to d-butaclamol, displacement of 3H-spiroperidol from rat striatal homogenates. The variation of composition of various polymers making compound 48/80 is suggested for explanation of obtained results.

Original languageEnglish (US)
Pages (from-to)359-363
Number of pages5
JournalPharmacology
Volume22
Issue number6
DOIs
StatePublished - Jan 1 1981

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p-Methoxy-N-methylphenethylamine
Opioid Receptors
Corpus Striatum
Morphine
Butaclamol
Spiperone
Vas Deferens
Enkephalins
Naloxone
Ileum
Analgesics
Polymers
Guinea Pigs

All Science Journal Classification (ASJC) codes

  • Pharmacology

Cite this

Janicki, Piotr ; Cztonkowski, A. ; Libich, J. ; Gumutka, S. W. / Lack of postulated opiate-receptor antagonistic properties of compound 48/80. In: Pharmacology. 1981 ; Vol. 22, No. 6. pp. 359-363.
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Lack of postulated opiate-receptor antagonistic properties of compound 48/80. / Janicki, Piotr; Cztonkowski, A.; Libich, J.; Gumutka, S. W.

In: Pharmacology, Vol. 22, No. 6, 01.01.1981, p. 359-363.

Research output: Contribution to journalArticle

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AB - The previously suggested opiate-receptor antagonistic properties of compound 48/80 were checked both in vivo and in vitro. In electrically stimulated guinea pig ileum and rat vas deferens preparations compound 48/80 did not reverse the inhibition of the twitches caused either by morphine or Met5-enkephalin. In mice hot-plate test compound 48/80 did not decrease the analgesic activity of morphine. In radioreceptor studies compound 48/80 shows rather low affinity to the 3H-naloxone receptor sites from striatal homogenates of the rat, as compared to non-labelled naloxone and on the other hand it produced moderate, as compared to d-butaclamol, displacement of 3H-spiroperidol from rat striatal homogenates. The variation of composition of various polymers making compound 48/80 is suggested for explanation of obtained results.

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