[Study of thermoregulatory activity of a fragment of natural dermorphin precursor Arg-dermorphin and its analogs]. 2005

T G Emel'ianova, and L S Guzevatykh, and N N Goriacheva, and L A Andreeva, and L Iu Alfeeva, and N F Miasoedov

We studied the effect of a fragment of natural dermorphin (DM) precursor Arg-DM and its analogs (Pro-DM, 4Amino-Pro-DM, Mike et-DM, Kre-DM, Arg-[DArg2]-DM, and Arg-[DAla4]-DM after intraperitoneal administration on the functional status of the thermoregulation system in rats. The obtained data demonstrated that the hypothermic and vasomotor effects of Arg-DM were temperature-dependent and had the same pattern as DM (Emel'yanova et al., 1996). In the thermoneutral and room environment, the peptide induced a two-phase vascular response. The first phase was vasodilation; it was twice as strong as for DM and was not removed by naloxone pretreatment. The second phase was vasoconstriction; it was blocked by naloxone. Replacement of Arg with 4Amino-Pro, Met, and Kre as well as DAla2 to DArg2 or Gly4 to DAla4 replacements in the Arg-DM molecule affected the thermoregulatory activity of the peptide. For instance, only the vasodilation response was observed for Arg-[DAla2]-DM and Arg-[DAla4]-DM while only the vasoconstriction response was observed for 4Amino-Pro-DM.

UI MeSH Term Description Entries
D008297 Male Males
D009842 Oligopeptides Peptides composed of between two and twelve amino acids. Oligopeptide
D011498 Protein Precursors Precursors, Protein
D001831 Body Temperature The measure of the level of heat of a human or animal. Organ Temperature,Body Temperatures,Organ Temperatures,Temperature, Body,Temperature, Organ,Temperatures, Body,Temperatures, Organ
D001833 Body Temperature Regulation The processes of heating and cooling that an organism uses to control its temperature. Heat Loss,Thermoregulation,Regulation, Body Temperature,Temperature Regulation, Body,Body Temperature Regulations,Heat Losses,Loss, Heat,Losses, Heat,Regulations, Body Temperature,Temperature Regulations, Body,Thermoregulations
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
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
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D014661 Vasoconstriction The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE. Vasoconstrictions
D014664 Vasodilation The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE. Vasodilatation,Vasorelaxation,Vascular Endothelium-Dependent Relaxation,Endothelium-Dependent Relaxation, Vascular,Relaxation, Vascular Endothelium-Dependent,Vascular Endothelium Dependent Relaxation

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