斯佩西亭

斯佩西亭（英语：Speciociliatine）^[2]是存在于卡痛树中主要生物碱，其为卡痛树中的另一种主要生物碱帽柱碱（英语：Mitragynine）的立体异构体。在干叶片中含量为0.00156- 2.9%。^[3][4]为一种阿片样肽受体配体。

斯佩西亭

法律规范状态
法律规范	美：未列入管制
识别信息
IUPAC命名法 methyl (E)-2-[(2S,3S,12bR)-3-ethyl-8-methoxy-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizin-2-yl]-3-methoxyprop-2-enoate
CAS号	14382-79-7
PubChem CID	5376107
ChemSpider	20124314
UNII	M3NN8Z8ZJW
ChEMBL	ChEMBL4546925
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID50574160
化学信息
化学式	C23H30N2O4
摩尔质量	398.50 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像
熔点	104 °C[1]
SMILES CC[C@@H]1CN2CCC3=C([C@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC
InChI InChI=1S/C23H30N2O4/c1-5-14-12-25-10-9-15-21-18(7-6-8-20(21)28-3)24-22(15)19(25)11-16(14)17(13-27-2)23(26)29-4/h6-8,13-14,16,19,24H,5,9-12H2,1-4H3/b17-13+/t14-,16+,19-/m1/s1 Key:LELBFTMXCIIKKX-MYLQJJOTSA-N

药理作用

已知斯佩西亭是μ-阿片样肽受体（英语：μ-opioid receptor）和κ-阿片样肽受体（英语：κ-opioid receptor）的配体，但其起到激动剂还是竞争拮抗剂作用目前存在争议。^[5][6]

在雄性实验大鼠身上测试表明，口服20 mg/kg斯佩西亭后，斯佩西亭的消除半衰期为2.6 - 5小时，绝对生物利用度为20.7%^[7]。

参考文献

1. National Center for Biotechnology Information (2022). PubChem Compound Summary for CID 15560576, Speciociliatine..
2. 苏子仁，赖小平. 汉英、英汉中草药化学成分词汇. 北京: 中国中医药出版社. 2006: 710. ISBN 9787801569103.
3. Sharma, A., Kamble, S. H., León, F., Chear, N. J. ‐Y., King, T. I., Berthold, E. C., Ramanathan, S., McCurdy, C. R., Avery, B. A., Simultaneous quantification of ten key Kratom alkaloids in Mitragyna speciosa leaf extracts and commercial products by ultra-performance liquid chromatography−tandem mass spectrometry, Drug Testing and Analysis (Wiley), 2019, 11 (8): 1162–1171, PMC 7927418 , PMID 30997725, doi:10.1002/dta.2604
4. Manwill, P. K., Flores-Bocanegra, L., Khin, M. Raja, H. A.; et al, Kratom (Mitragyna speciosa) Validation: Quantitative Analysis of Indole and Oxindole Alkaloids Reveals Chemotypes of Plants and Products, Planta Medica (Georg Thieme Verlag KG), 2022, 88 (9/10): 838–857, PMC 9343938 , PMID 35468648, doi:10.1055/a-1795-5876 引文格式1维护：显式使用等标签 (link)
5. Obeng, S., Kamble, S. H., Reeves, M. E.; et al, Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids, Journal of Medicinal Chemistry (American Chemical Society (ACS)), 2019, 63 (1): 433–439, PMC 7676998 , PMID 31834797, doi:10.1021/acs.jmedchem.9b01465 引文格式1维护：显式使用等标签 (link)
6. Kruegel, A. C., Gassaway, M. M., Kapoor, A; et al, Synthetic and Receptor Signaling Explorations of the Mitragyna Alkaloids: Mitragynine as an Atypical Molecular Framework for Opioid Receptor Modulators, Journal of the American Chemical Society (American Chemical Society (ACS)), 2016, 138 (21): 6754–6764, PMC 5189718 , PMID 27192616, doi:10.1021/jacs.6b00360 引文格式1维护：显式使用等标签 (link)
7. Berthold, E. C., Kamble, S. H., Raju, K. S.; et al, Preclinical pharmacokinetic study of speciociliatine, a kratom alkaloid, in rats using an UPLC-MS/MS method, Journal of Pharmaceutical and Biomedical Analysis (Elsevier BV), 2021, 194: 113778, PMID 33277117, S2CID 227296714, doi:10.1016/j.jpba.2020.113778 引文格式1维护：显式使用等标签 (link)