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Inhibition of gastrointestinal transit by morphine and FK 33-824 in the rat and comparative narcotic antagonist properties of naloxone and its N-methyl quaternary analog.

Abstract：

:Morphine and the enkephalin-like peptide FK 33-824 given i.p. to rats potently inhibit gastrointestinal transit of a charcoal test meal, the doses inhibiting transit by 50% being respectively about 10 and 1 microgram/kg. These intestinal effects are opiate-specific, locally elicited and presumably involve the same action site since they are reversed by the "peripherally selective" narcotic antagonist N-methyl naloxone with apparent pA2 values of 7.34 and 7.10 respectively against morphine and FK 33-824. The calculated pA2 value for naloxone/morphine with the same in vivo test procedure (8.83) and the relative ability of naloxone and N-methyl naloxone to prevent 3H-etorphine binding to rat brain membranes (IC50 43 and 541 nM), indicate different potency ratios between the two narcotic antagonists in the in vitro binding cell-free system (about 1:10) and in vivo (about 1:30), but the latter ratio agrees with published findings in the isolated guinea pig ileum.

journal_name

Life Sci

journal_title

Life sciences

authors

Manara L,Bianchi G,Fiocchi R,Notarnicola A,Peracchia F,Tavani A

doi

10.1016/0024-3205(82)90359-9

subject

Has Abstract

pub_date

1982-09-20 00:00:00

pages

1271-4

issue

12-13

eissn

0024-3205

issn

1879-0631

pii

0024-3205(82)90359-9

journal_volume

31

pub_type

杂志文章

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