[Effects of the dynorphin derivative "E2078" on hemodynamics and plasma catecholamines in dogs]. 1990

K Hirota
Department of Anesthesiology, University of Hirosaki School of Medicine.

Recently, a dynorphin derivative (E2078) is synthesized as a kappa-agonist. Unlike dynorphin, E2078 is easily inactivated by peptidases. In this study, hemodynamic effects of E2078 were investigated in 54 adult mongrel dogs under enflurane anesthesia. They were divided into 6 groups according to the dose of E2078 administrated. In the small dosage groups (0.05, 0.1 mg.kg-1), systemic blood pressure was reduced due to cardiac depression. In the large dosage groups (1.0 mg.kg-1, 10 mg.kg-1), the systemic blood pressure decreased due to vasodilation while the cardiac output increased. In the 1.0 mg.kg-1 group, the heart rate decreased, but it increased in the 10 mg.kg-1 group. This difference could be caused by decreased plasma catecholamines in the 1.0 mg.kg-1 group, and their increase in the 10 mg.kg-1 group. The changes in plasma catecholamine levels might be a factor contributing to circulatory depression due to decreased norepinephrine release from the sympathetic nerve endings by E2078 as observed following administration of other kappa-ligands. Another factor for hemodynamic depression would be a direct action of E2078 to dilate vascular bed.

UI MeSH Term Description Entries
D010446 Peptide Fragments Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques. Peptide Fragment,Fragment, Peptide,Fragments, Peptide
D002395 Catecholamines A general class of ortho-dihydroxyphenylalkylamines derived from TYROSINE. Catecholamine,Sympathin,Sympathins
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
D004399 Dynorphins A class of opioid peptides including dynorphin A, dynorphin B, and smaller fragments of these peptides. Dynorphins prefer kappa-opioid receptors (RECEPTORS, OPIOID, KAPPA) and have been shown to play a role as central nervous system transmitters. Dynorphin,Dynorphin (1-17),Dynorphin A,Dynorphin A (1-17)
D006439 Hemodynamics The movement and the forces involved in the movement of the blood through the CARDIOVASCULAR SYSTEM. Hemodynamic
D000700 Analgesics Compounds capable of relieving pain without the loss of CONSCIOUSNESS. Analgesic,Anodynes,Antinociceptive Agents,Analgesic Agents,Analgesic Drugs,Agents, Analgesic,Agents, Antinociceptive,Drugs, Analgesic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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