1981
DOI: 10.1016/0024-3205(81)90297-6
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Opioid activities of β-casomorphins

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Cited by 215 publications
(72 citation statements)
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“…There are at least two observations that are relevant in this regard: 1) P-casomorphin-5 and 7 and morphiceptin (Tyr-Pro-Phe-Pro-NH2) can be cleaved from larger molecules such as BCMIR in the blood or other tissues such as brain (3), and 2) these shorter P-casomorphins are well known selective and powerful popioid agonists (4,18). Whether BCMIR itself has opioid activity is not known, but its cleavage products do (2,3).…”
Section: Discussionmentioning
confidence: 99%
“…There are at least two observations that are relevant in this regard: 1) P-casomorphin-5 and 7 and morphiceptin (Tyr-Pro-Phe-Pro-NH2) can be cleaved from larger molecules such as BCMIR in the blood or other tissues such as brain (3), and 2) these shorter P-casomorphins are well known selective and powerful popioid agonists (4,18). Whether BCMIR itself has opioid activity is not known, but its cleavage products do (2,3).…”
Section: Discussionmentioning
confidence: 99%
“…The results can be summarized as follows: (i) Proteolytic enzymes of gastrointestinal tract plus Ieucine aminopeptidase, under controlled conditions, do not release ~-casomorphin 7 from &casein but a putative precursor, i.e., procasomorphin; (ii) Procasomorphin is further digested by brush border peptidases but not to casomorphin; (iii) The peptide Tyr-Pro-Phe still resistant to proteolytic activity of the brush border is devoid of any opioid activity [9]. Apparently our results seem then to exclude a physiological role for ,&casomorphin.…”
Section: Brush Border Digestmentioning
confidence: 96%
“…Sur la base du test «dit» du retrait de la queue des souris après pincement, l'injection intracérébroventriculaire des différentes j3-casomorphinesa permis de quantifier leur activité antidouleur, non seulement entre elles, mais aussi par rapport à la morphine. Par exemple, la j3-casomorphine 1-5 est de 10 à 20 fois moins active que la morphine (Brantl et al, 1981), bien qu'il suffise de 0,06 à 2 J1 mole par rat pour obtenir un effet analgé-sique appréciable; en revanche, la j3-casomorphine 1-4 NH 2 , appelée encore morphiceptine, modifiée par substitution des acinés L par position 2 et 4 par des acides aminés D ou par de l'acide D pipé-colique serait 10 fois plus active que la morphine (Chang et al, 1982). La formation au niveau de l'intestin grêle de la morphiceptine semble hautement probable, puisqu'une réaction positive est observée avec un anticorps spécifique et que des enzymes d'amidation existent dans le tractus gastro-intestinal et dans le suc pancréatique (Chang et al, 1985).…”
Section: Peptides à Activité Opiacéeunclassified