Takayanagi I, Okumura K, Konno F, Koike K, Cho N, Hirobe M
Gen Pharmacol. 1985;16(6):617-9. doi: 10.1016/0306-3623(85)90153-3.
Nalorphine and nalorphine-7,8-oxide (nalorphine epoxide) behaved as partial agonists on the kappa-receptor in the electrically stimulated mouse vas deferens. The effects of a GTP-analogue, GppNHp and Na+ on the inhibition of [3H]ethylketocyclazocine binding by dynorphin 1-13, nalorphine, its epoxide and naloxone (antagonist) were studied with a synaptosomal fraction of guinea pig brain (except a cerebellum) and compared with the intrinsic activity of the test drugs, which was estimated in the electrically stimulated mouse vas deferens. The effects of GppNHp and Na+ on the affinity of the drugs to the kappa-receptor correlated with their intrinsic activities.
纳洛啡和纳洛啡 - 7,8 - 氧化物（纳洛啡环氧化物）在电刺激的小鼠输精管中对κ受体表现为部分激动剂。用豚鼠脑（小脑除外）的突触体部分研究了GTP类似物GppNHp和Na⁺对强啡肽1 - 13、纳洛啡、其环氧化物和纳洛酮（拮抗剂）抑制[³H]乙基酮环唑新结合的影响，并与在电刺激的小鼠输精管中估计的受试药物的内在活性进行了比较。GppNHp和Na⁺对药物与κ受体亲和力的影响与其内在活性相关。
