Sugden D
Biomedical Sciences Division, King's College London, U.K.
Eur J Pharmacol. 1992 Mar 31;213(3):405-8. doi: 10.1016/0014-2999(92)90629-i.
The ability of putative melatonin receptor antagonists to antagonise melatonin-induced aggregation of pigment granules in cultured neural crest Xenopus laevis melanophores was examined. Neither ML 23 (N-(2,4-dinitrophenyl)-5-methoxytryptamine) nor 6-methoxy-2-benzoxazolinone showed agonist or antagonist activity. N-Acetyltryptamine and N-butanoyltryptamine were partial agonists; both compounds aggregated pigment granules in some cells, but also reversed melatonin-induced pigment agreggation in a fraction of the cells tested. In contrast, 2-benzyl N-acetyltryptamine (luzindole) did not show agonist activity (upto 10 microM) but did reverse the aggregating action of melatonin at 1 and 10 microM. Pretreatment of melanophores with luzindole shifted the melatonin concentration-response curve to the right.
研究了假定的褪黑素受体拮抗剂拮抗褪黑素诱导培养的非洲爪蟾神经嵴黑素细胞中色素颗粒聚集的能力。ML 23(N-(2,4-二硝基苯基)-5-甲氧基色胺)和6-甲氧基-2-苯并恶唑啉酮均未表现出激动剂或拮抗剂活性。N-乙酰色胺和N-丁酰色胺是部分激动剂;这两种化合物在一些细胞中使色素颗粒聚集,但在一部分测试细胞中也能逆转褪黑素诱导的色素聚集。相比之下,2-苄基N-乙酰色胺(鲁辛朵)在高达10微摩尔时未表现出激动剂活性,但在1微摩尔和10微摩尔时能逆转褪黑素的聚集作用。用鲁辛朵预处理黑素细胞可使褪黑素浓度-反应曲线右移。