C0331
6-氯褪黑激素
别名:
N-乙酰基-6-氯-5-甲氧基色胺
溶解性
alcohol: soluble
储存温度
2-8°C
SMILES字符串
COc1cc2c(CCNC(C)=O)c[nH]c2cc1Cl
基因信息
human ... MTNR1A(4543), MTNR1B(4544)
生化/生理作用
纳摩尔浓度级褪黑激素激动剂活性物质；受体结合能力比褪黑激素更强。在 CNS 外也有结合位点，例如肾上腺的结合位点。具有抗增殖活性。
法规信息
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S W Ying et al.
European journal of pharmacology, 246(2), 89-96 (1993-07-15)
In order to explore the potential oncostatic properties of the pineal hormone, melatonin, we have investigated its binding characteristics and functional effects in a human malignant melanoma (M-6) cell line. Binding studies in M-6 membranes showed the coexistence of 2-[125I]iodomelatonin
S P Persengiev
Life sciences, 51(9), 647-651 (1992-01-01)
Specific binding sites for 2-[125I] iodomelatonin, a selective radiolabeled melatonin receptor ligand, were detected and characterized in rat adrenal membranes. Saturation studies demonstrated that 2-[125I]iodomelatonin binds to a single class of sites with an affinity constant (Kd) of 541 pM
C Browning et al.
British journal of pharmacology, 129(5), 877-886 (2000-03-01)
We have pharmacologically characterized recombinant human mt(1) and MT(2) receptors, stably expressed in Chinese hamster ovary cells (CHO-mt(1) and CHO-MT(2)), by measurement of [(3)H]-melatonin binding and forskolin-stimulated cyclic AMP (cAMP) production. [3H]-melatonin bound to mt(1) and MT(2) receptors with pK(D)
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