Feuerstein G, Zukowska-Grojec Z
Neuropeptides. 1987 Feb-Mar;9(2):139-50. doi: 10.1016/0143-4179(87)90052-7.
Dermorphin is a recently discovered opioid peptide which is unique in having a D-amino acid in its sequence. Dermorphin binding sites have been shown in central and peripheral organs and central administered dermorphin produces profound autonomic responses. The purpose of this study was to examine the effect of intravenous dermorphin on heart rate and blood pressure of the pithed rat in basal condition and in response to controlled sympathetic stimulation. Also, since dermorphin is a selective mu-receptor agonist, its effects were compared to morphine, an opiate selective for mu receptors. Dermorphin (0.0001-10 mumol/kg, i.v) or morphine (1-10 mg/kg) had no effect on basal heart rate or blood pressure and failed to modify sympatho-adreno-medullary evoked pressor and tachycardic responses. Furthermore, dermorphin or morphine did not affect the increase in plasma norepinephrine and epinephrine in response to spinal cord stimulation. It is concluded that the dermorphin and morphine have no direct peripheral effects on heart rate or blood vessel tone nor do these mu-receptor agonists have any effect on norepinephrine and epinephrine release from the sympathetic nerves and the adrenal medulla in the rat.
强啡肽是一种最近发现的阿片肽，其独特之处在于其序列中含有一个D-氨基酸。已在中枢和外周器官中显示出强啡肽结合位点，并且中枢给予强啡肽会产生深刻的自主反应。本研究的目的是研究静脉注射强啡肽对基础状态下以及对受控交感神经刺激有反应的去大脑大鼠的心率和血压的影响。此外，由于强啡肽是一种选择性μ受体激动剂，将其作用与吗啡（一种对μ受体有选择性的阿片类药物）的作用进行了比较。强啡肽（0.0001-10μmol/kg，静脉注射）或吗啡（1-10mg/kg）对基础心率或血压没有影响，并且未能改变交感-肾上腺髓质诱发的升压和心动过速反应。此外，强啡肽或吗啡不影响脊髓刺激引起的血浆去甲肾上腺素和肾上腺素的增加。得出的结论是，强啡肽和吗啡对心率或血管张力没有直接的外周作用，并且这些μ受体激动剂对大鼠交感神经和肾上腺髓质释放去甲肾上腺素和肾上腺素也没有任何影响。
