Synthesis and receptor binding activity of elephant beta-endorphin, a beta-endorphin homolog with highly potent analgesic activity.
Synthesis and receptor binding activity of elephant beta-endorphin, a beta-endorphin homolog with highly potent analgesic activity.
复制标题
大象β-内啡肽（一种具有高效镇痛活性的β-内啡肽同系物）的合成和受体结合活性。
DOI：
10.1111/j.1399-3011.1991.tb01411.x
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发表时间：
1991
期刊：
影响因子：
--
通讯作者：
Yamashiro,D
中科院分区：
文献类型：
--
作者：
Cheng,HC;Yamashiro,D
采用标准固相法合成了大象β -内啡肽及其类似物大象β -内啡肽（6 - 31）。受体结合活性表明，大象β -内啡肽与大鼠脑膜上阿片受体的结合能力是人β -内啡肽的5 ~ 6倍。在之前的研究中(Wong， C.‐L.；王伟，m - K。，程，H. - C.；， Chung， D.和Yamashiro， D.（1990）临床和实验药理学和生理学（16,33-37），脑室内注射β -内啡肽的摇尾试验表明，大象β -内啡肽在小鼠中的抗伤害性效力比人类β -内啡肽高7 - 8倍。两项研究结果均表明，在甩尾实验中，大象β -内啡肽比人β -内啡肽具有更强的抗痛觉活性，其镇痛活性可能与大象β -内啡肽对脑内阿片受体的亲和力有关。
Elephant β‐endorphin and its analog, elephant β‐endorphin(6‐31) were synthesized by standard solid phase method. Receptor binding activity showed that elephant β‐endorphin was five to six times more potent than human β‐endorphin in its ability to bind to opiate receptors on rat brain membrane. In a previous study (Wong, C.‐L., Wai, M.‐K., Cheng, H.‐C., Chung, D. & Yamashiro, D (1990)Clinical and Experimental Pharmacology and Physiology16, 33–37), tail flick test for intracerebroventricularly administered β‐endor‐phin showed that the antinociceptive potency of elephant β‐endorphin was seven to eight times higher than that of human β‐endorphin in mice. Results from both studies suggest that elephant β‐endorphin was a much more potent antinociceptive agent than human β‐endorphin in tail flick test and its higher analgesic activity might be due to its higher affinity for opiate receptors in the brain.