Effect of β-casomorphins on intestinal propulsion in the guinea-pig colon

F. De Ponti, M. Marcoli, S. Lecchini, L. Manzo, G. M. Frigo, A. Crema

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

β-Casomorphins are a family of opioid peptides originally isolated from β-casein. In view of a possible physiological significance of these milk-derived compounds, the effects of bovine β-casomorphin-5 (β-CM-5), β-casomorphin-4 (β-CM-4) and D-Ala2-β-casomorphin-4-NH2 (D-Ala2-β-CM-4-NH2) have been investigated on the peristaltic reflex in the guinea-pig isolated colon and compared with morphine. β-CM-5 and D-Ala2-β-CM-4-NH2 each dose-dependently inhibited the velocity of propulsion of an intraluminal bolus; β-CM-4 was ineffective. IC50 values were 0.30, 5.21 and 0.29 μM for morphine, β-CM-5 and D-Ala2-β-CM-NH2, respectively. The potency ratios vs morphine were 0.06 and 0.96 for β-CM-5 and D-Ala2-β-CM-4-NH2, respectively. Blockade of the peristaltic reflex by β-CM-5 or D-Ala2-β-CM-4-NH2 was reversed by the opioid antagonist naloxone. D-Ala2-β-CM-4-NH2 also dose-dependently inhibited resting acetylcholine output (IC50 = 5.69 μM; potency ratio vs morphine: 0.63). In conclusion, certain β-casomorphins inhibit intestinal propulsion and cholinergic neurotransmission in the guinea-pig colon, probably by acting at opioid receptors.

Original languageEnglish
Pages (from-to)302-305
Number of pages4
JournalJournal of Pharmacy and Pharmacology
Volume41
Issue number5
Publication statusPublished - 1989

Fingerprint

Morphine
Guinea Pigs
Colon
Inhibitory Concentration 50
Reflex
Opioid Peptides
Narcotic Antagonists
Opioid Receptors
Naloxone
Caseins
Synaptic Transmission
Cholinergic Agents
Acetylcholine
Milk

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Pharmacology

Cite this

De Ponti, F., Marcoli, M., Lecchini, S., Manzo, L., Frigo, G. M., & Crema, A. (1989). Effect of β-casomorphins on intestinal propulsion in the guinea-pig colon. Journal of Pharmacy and Pharmacology, 41(5), 302-305.

Effect of β-casomorphins on intestinal propulsion in the guinea-pig colon. / De Ponti, F.; Marcoli, M.; Lecchini, S.; Manzo, L.; Frigo, G. M.; Crema, A.

In: Journal of Pharmacy and Pharmacology, Vol. 41, No. 5, 1989, p. 302-305.

Research output: Contribution to journalArticle

De Ponti, F, Marcoli, M, Lecchini, S, Manzo, L, Frigo, GM & Crema, A 1989, 'Effect of β-casomorphins on intestinal propulsion in the guinea-pig colon', Journal of Pharmacy and Pharmacology, vol. 41, no. 5, pp. 302-305.
De Ponti F, Marcoli M, Lecchini S, Manzo L, Frigo GM, Crema A. Effect of β-casomorphins on intestinal propulsion in the guinea-pig colon. Journal of Pharmacy and Pharmacology. 1989;41(5):302-305.
De Ponti, F. ; Marcoli, M. ; Lecchini, S. ; Manzo, L. ; Frigo, G. M. ; Crema, A. / Effect of β-casomorphins on intestinal propulsion in the guinea-pig colon. In: Journal of Pharmacy and Pharmacology. 1989 ; Vol. 41, No. 5. pp. 302-305.
@article{07b3bc68aab9457489a3d2d5217cf424,
title = "Effect of β-casomorphins on intestinal propulsion in the guinea-pig colon",
abstract = "β-Casomorphins are a family of opioid peptides originally isolated from β-casein. In view of a possible physiological significance of these milk-derived compounds, the effects of bovine β-casomorphin-5 (β-CM-5), β-casomorphin-4 (β-CM-4) and D-Ala2-β-casomorphin-4-NH2 (D-Ala2-β-CM-4-NH2) have been investigated on the peristaltic reflex in the guinea-pig isolated colon and compared with morphine. β-CM-5 and D-Ala2-β-CM-4-NH2 each dose-dependently inhibited the velocity of propulsion of an intraluminal bolus; β-CM-4 was ineffective. IC50 values were 0.30, 5.21 and 0.29 μM for morphine, β-CM-5 and D-Ala2-β-CM-NH2, respectively. The potency ratios vs morphine were 0.06 and 0.96 for β-CM-5 and D-Ala2-β-CM-4-NH2, respectively. Blockade of the peristaltic reflex by β-CM-5 or D-Ala2-β-CM-4-NH2 was reversed by the opioid antagonist naloxone. D-Ala2-β-CM-4-NH2 also dose-dependently inhibited resting acetylcholine output (IC50 = 5.69 μM; potency ratio vs morphine: 0.63). In conclusion, certain β-casomorphins inhibit intestinal propulsion and cholinergic neurotransmission in the guinea-pig colon, probably by acting at opioid receptors.",
author = "{De Ponti}, F. and M. Marcoli and S. Lecchini and L. Manzo and Frigo, {G. M.} and A. Crema",
year = "1989",
language = "English",
volume = "41",
pages = "302--305",
journal = "Journal of Pharmacy and Pharmacology",
issn = "0022-3573",
publisher = "Pharmaceutical Press",
number = "5",

}

TY - JOUR

T1 - Effect of β-casomorphins on intestinal propulsion in the guinea-pig colon

AU - De Ponti, F.

AU - Marcoli, M.

AU - Lecchini, S.

AU - Manzo, L.

AU - Frigo, G. M.

AU - Crema, A.

PY - 1989

Y1 - 1989

N2 - β-Casomorphins are a family of opioid peptides originally isolated from β-casein. In view of a possible physiological significance of these milk-derived compounds, the effects of bovine β-casomorphin-5 (β-CM-5), β-casomorphin-4 (β-CM-4) and D-Ala2-β-casomorphin-4-NH2 (D-Ala2-β-CM-4-NH2) have been investigated on the peristaltic reflex in the guinea-pig isolated colon and compared with morphine. β-CM-5 and D-Ala2-β-CM-4-NH2 each dose-dependently inhibited the velocity of propulsion of an intraluminal bolus; β-CM-4 was ineffective. IC50 values were 0.30, 5.21 and 0.29 μM for morphine, β-CM-5 and D-Ala2-β-CM-NH2, respectively. The potency ratios vs morphine were 0.06 and 0.96 for β-CM-5 and D-Ala2-β-CM-4-NH2, respectively. Blockade of the peristaltic reflex by β-CM-5 or D-Ala2-β-CM-4-NH2 was reversed by the opioid antagonist naloxone. D-Ala2-β-CM-4-NH2 also dose-dependently inhibited resting acetylcholine output (IC50 = 5.69 μM; potency ratio vs morphine: 0.63). In conclusion, certain β-casomorphins inhibit intestinal propulsion and cholinergic neurotransmission in the guinea-pig colon, probably by acting at opioid receptors.

AB - β-Casomorphins are a family of opioid peptides originally isolated from β-casein. In view of a possible physiological significance of these milk-derived compounds, the effects of bovine β-casomorphin-5 (β-CM-5), β-casomorphin-4 (β-CM-4) and D-Ala2-β-casomorphin-4-NH2 (D-Ala2-β-CM-4-NH2) have been investigated on the peristaltic reflex in the guinea-pig isolated colon and compared with morphine. β-CM-5 and D-Ala2-β-CM-4-NH2 each dose-dependently inhibited the velocity of propulsion of an intraluminal bolus; β-CM-4 was ineffective. IC50 values were 0.30, 5.21 and 0.29 μM for morphine, β-CM-5 and D-Ala2-β-CM-NH2, respectively. The potency ratios vs morphine were 0.06 and 0.96 for β-CM-5 and D-Ala2-β-CM-4-NH2, respectively. Blockade of the peristaltic reflex by β-CM-5 or D-Ala2-β-CM-4-NH2 was reversed by the opioid antagonist naloxone. D-Ala2-β-CM-4-NH2 also dose-dependently inhibited resting acetylcholine output (IC50 = 5.69 μM; potency ratio vs morphine: 0.63). In conclusion, certain β-casomorphins inhibit intestinal propulsion and cholinergic neurotransmission in the guinea-pig colon, probably by acting at opioid receptors.

UR - http://www.scopus.com/inward/record.url?scp=0024349530&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0024349530&partnerID=8YFLogxK

M3 - Article

VL - 41

SP - 302

EP - 305

JO - Journal of Pharmacy and Pharmacology

JF - Journal of Pharmacy and Pharmacology

SN - 0022-3573

IS - 5

ER -