Synthesis and receptor binding activity of elephant beta-endorphin, a beta-endorphin homolog with highly potent analgesic activity.
Elephant beta-endorphin and its analog, elephant beta-endorphin(6-31) were synthesized by standard solid phase method. Receptor binding activity showed that elephant beta-endorphin was five to six times more potent than human beta-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 Physiology 16, 33-37), tail flick test for intracerebroventricularly administered beta-endorphin showed that the antinociceptive potency of elephant beta-endorphin was seven to eight times higher than that of human beta-endorphin in mice. Results from both studies suggest that elephant beta-endorphin was a much more potent antinociceptive agent than human beta-endorphin in tail flick test and its higher analgesic activity might be due to its higher affinity for opiate receptors in the brain.
Cheng
H C
HC
Department of Medical Biochemistry, Faculty of Medicine, University of Calgary, Canada.
Yamashiro
D
D
D000595:Amino Acid Sequence; D000700:Analgesics; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004606:Elephants; D006801:Humans; D008969:Molecular Sequence Data; D051381:Rats; D011957:Receptors, Opioid / Q000378:metabolism*; D001615:beta-Endorphin / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism*
D000700:Analgesics; D011957:Receptors, Opioid; D001615:beta-Endorphin