M&B 28,767: a potent anti-secretory and anti-ulcer PG analogue. A comparative study with 16, 16' dimethyl PGE2 methylester.

M&B 28,767 [(+/-)11-deoxy-16-phenoxy-omega-tetranor PGE1] and 16, 16'-dimethyl PGE2 methylester (DMPG) were compared for their effects on gastric acid secretion (GAS) and gastric ulceration (GU), employing various laboratory models. In anaesthetised rats, GAS was stimulated by a continuous i.v. infusion of pentagastrin (30 micrograms/kg/h), and PG analogues were perfused through the stomach for 1 h. M&B 28,767 (3-15 micrograms/kg/h) and DMPG (3-60 micrograms/kg/h) reduced GAS in a dose-related manner, the ED50 values being 4 and 15 micrograms/kg/h respectively. In conscious rats possessing indwelling gastric cannulae, oral doses of M&B 28,767 (0.025-0.1 microgram/kg) and DMPG (0.50-1.0 microgram/kg) caused a prolonged inhibition of pentagastrin-stimulated GAS. M&B 28,767 was 17 times more potent than DMPG; the respective ED50 values were 0.036 and 0.6 microgram/kg. Indomethacin-induced ulceration in rats, was reduced by both M&B 28,767 and DMPG; the respective ED50 values being 3.0 and 0.8 micrograms/kg. Both compounds given orally increased gastrointestinal motility in mice; M&B 28,767 (1-3 mg/kg) and DMPG (0.1-0.3 mg/kg) caused diarrhoea, the former being about 0.1 times as potent as the latter. In another test, M&B 28,767 (0.5-5.0 mg/kg) and DMPG (10-40 micrograms/kg) overcame morphine-induced constipation in a dose-related manner, the respective ED50s being 0.9-1.4 mg/kg and 20-40 micrograms/kg. Thus, M&B 28,767 had a better profile of activity than DMPG as an antisecretory and antiulcer agent.
AuthorsA K Banerjee, A J Christmas, K Crowshaw, M A Heazell, G C Ivers-Read, L C Saunders, D Wyatt
JournalLife sciences (Life Sci) Vol. 35 Issue 25 Pg. 2489-96 (Dec 17 1984) ISSN: 0024-3205 [Print] ENGLAND
PMID6513724 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Prostaglandins E, Synthetic
  • Morphine
  • 11-deoxy-16-phenoxy-17,18,19,20-tetranorprostaglandin E1
  • Pentagastrin
  • Alprostadil
  • 16,16-Dimethylprostaglandin E2
  • Indomethacin
  • 16,16-Dimethylprostaglandin E2 (pharmacology)
  • Alprostadil (analogs & derivatives)
  • Animals
  • Constipation (chemically induced)
  • Diarrhea (chemically induced)
  • Gastric Acid (secretion)
  • Gastrointestinal Motility (drug effects)
  • Indomethacin (pharmacology)
  • Male
  • Mice
  • Morphine (pharmacology)
  • Pentagastrin (pharmacology)
  • Prostaglandins E, Synthetic (pharmacology)
  • Rats
  • Rats, Inbred Strains
  • Stomach Ulcer (chemically induced, prevention & control)

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