Clark W G, Bernardini G L, Ponder S W
Pharmacol Biochem Behav. 1982 Jun;16(6):989-93. doi: 10.1016/0091-3057(82)90058-2.
FK 33-824 [H2N-Tyr-D-Ala-Gly-MePhe-Met(O)-OH] was injected into the third cerebral ventricle of unrestrained cats. Doses of 0.25-4 microgram induced dose-related increases in body temperature. Hyperthermic responses to 1 microgram of the peptide were greater the warmer the environment. Naloxone given intraventricularly 1 hr after FK 33-824 (1 microgram) reduced the hyperthermia. In 12 tests with six cats FK 33-824 (1-25 microgram) increased temperature 4.2-4.7 degrees C. These marked responses were also inhibited by naloxone, but two cats died when administration of antagonist was delayed for 80 min to 3 hr after attainment of maximal body temperature. Larger doses of FK 33-824 (50-250 microgram) evoked little increase in temperature, indicative of a separate action to depress thermoregulation. Although responses to FK 33-824 were antagonized by naloxone, this peptide, like another enkephalin analog D-Ala2-Met-enkephalinamide, must act on receptors which are not affected by morphine since (1) the hyperthermic response to FK 33-824 varied with environmental temperature, whereas the response to morphine does not, and (2) high doses of FK 33-824 depressed thermoregulation, an activity not shared by morphine in the cat. Furthermore, the maximal increases in temperature after FK 33-824 injection were greater than those evoked by either morphine or D-Ala2-Met-enkephalinamide. This observation provides evidence for an additional subset of naloxone-sensitive, v, receptors, stimulation of which can influence thermoregulation in the cat.
将FK 33 - 824 [H2N - Tyr - D - Ala - Gly - MePhe - Met(O) - OH]注入未受限制的猫的第三脑室。剂量为0.25 - 4微克时可引起体温呈剂量相关的升高。环境温度越高,对1微克该肽的热反应就越大。在给予FK 33 - 824(1微克)1小时后脑室内注射纳洛酮可降低体温过高。在用6只猫进行的12次试验中,FK 33 - 824(1 - 25微克)使体温升高4.2 - 4.7摄氏度。这些明显的反应也被纳洛酮抑制,但当在体温达到最高值后80分钟至3小时延迟给予拮抗剂时,有两只猫死亡。更大剂量的FK 33 - 824(50 - 250微克)引起的体温升高很少,表明其有单独的抑制体温调节的作用。尽管对FK 33 - 824的反应被纳洛酮拮抗,但该肽与另一种脑啡肽类似物D - Ala2 - Met - 脑啡肽酰胺一样,必定作用于不受吗啡影响的受体,因为(1)对FK 33 - 824的热反应随环境温度而变化,而对吗啡的反应则不然;(2)高剂量的FK 33 - 824抑制体温调节,而吗啡在猫中不具有这种活性。此外,注射FK 33 - 824后体温的最大升高幅度大于吗啡或D - Ala2 - Met - 脑啡肽酰胺所引起的升高幅度。这一观察结果为纳洛酮敏感的、v型受体的另一个亚群提供了证据,刺激该亚群可影响猫的体温调节。