Enterostatin (APGPR) suppresses the analgesic activity of morphine by a CCK-dependent mechanism.
Enterostatin (APGPR) found in the gastrointestinal tract and brain is an anorectic pentapeptide. We found that APGPR inhibited morphine-induced analgesia after intracerebroventricular administration in mice at a dose of 10nmol/mouse. The anti-analgesic effect of APGPR was inhibited by pretreatment with lorglumide and LY225910, antagonists for cholecystokinin 1 (CCK1) and cholecystokinin 2 (CCK2) receptors, respectively. The anti-analgesic effect of APGPR may be mediated by CCK release, since APGPR does not have affinity for CCK receptors.
Takenaka
Yasuyuki
Y
Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University, Uji, Kyoto 611-0011, Japan.
Shimano
Tomoko
T
Yamada
Yuko
Y
Yoshida
Mariko
M
Ohinata
Kousaku
K
Yoshikawa
Masaaki
M
D000700:Analgesics / Q000037:antagonists & inhibitors*; D000818:Animals; D002766:Cholecystokinin / Q000378:metabolism*; D003089:Colipases / Q000494:pharmacology*; D004792:Enzyme Precursors / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009020:Morphine / Q000037:antagonists & inhibitors*; D011949:Receptors, Cholecystokinin / Q000378:metabolism
D000700:Analgesics; D003089:Colipases; D004792:Enzyme Precursors; D011949:Receptors, Cholecystokinin; C037107:procolipase; D009020:Morphine; D002766:Cholecystokinin