Pharmacology of a gut motility stimulating enkephalin analogue. 1985

M Bickel, and H G Alpermann, and M Roche, and M Schemann, and H J Ehrlein

The enkephalin analogue pentapeptide Hoe 825 (Tyr-D-Lys-Gly-Phe-L-homocysteine-thiolactone) is a mixed mu/delta opiate agonist. The peptide stimulated interdigestive gut motility at all parts of the intestine in conscious and anaesthetized animals. In dogs digestive motility, measuring mechanical activity, was stimulated with respect to segmental and propulsive properties. The canine uterus was sensitive to the enkephalin. Hoe 825 acts by i.v. or s.c. application, whereas the latter increases the duration of action significantly. The compound's effect can be blocked by naloxone indicating a receptor mediated action, which is localised peripherally. The compound is devoid of a dependence risk, because it does not penetrate into the CNS. At therapeutic doses (in the dog 0.5-2 micrograms/kg i.v.) the compound does not affect cardiovascular, renal or endocrine functions and was without effect on serum blood glucose levels in rats and rabbits.

UI MeSH Term Description Entries
D007413 Intestinal Mucosa Lining of the INTESTINES, consisting of an inner EPITHELIUM, a middle LAMINA PROPRIA, and an outer MUSCULARIS MUCOSAE. In the SMALL INTESTINE, the mucosa is characterized by a series of folds and abundance of absorptive cells (ENTEROCYTES) with MICROVILLI. Intestinal Epithelium,Intestinal Glands,Epithelium, Intestinal,Gland, Intestinal,Glands, Intestinal,Intestinal Gland,Mucosa, Intestinal
D007668 Kidney Body organ that filters blood for the secretion of URINE and that regulates ion concentrations. Kidneys
D008297 Male Males
D009842 Oligopeptides Peptides composed of between two and twelve amino acids. Oligopeptide
D011919 Rats, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D001786 Blood Glucose Glucose in blood. Blood Sugar,Glucose, Blood,Sugar, Blood
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D004285 Dogs The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065) Canis familiaris,Dog
D005260 Female Females
D005769 Gastrointestinal Motility The motor activity of the GASTROINTESTINAL TRACT. Intestinal Motility,Gastrointestinal Motilities,Intestinal Motilities,Motilities, Gastrointestinal,Motilities, Intestinal,Motility, Gastrointestinal,Motility, Intestinal

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