斯佩西亭（英語：Speciociliatine）[2]是存在於卡痛樹中主要生物鹼，其為卡痛樹中的另一種主要生物鹼帽柱鹼的立體異構體。在干葉片中含量為0.00156- 2.9%。[3][4]為一種阿片樣肽受體配體。
Quick Facts 法律規範狀態, 法律規範 ...
斯佩西亭 |
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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
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| CAS號 | 14382-79-7 |
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| 化學式 | C23H30N2O4 |
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| 摩爾質量 | 398.50 g·mol−1 |
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| 3D模型（JSmol） | |
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| 熔點 | 104 °C[1] |
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CC[C@@H]1CN2CCC3=C([C@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC
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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
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已知斯佩西亭是μ-阿片樣肽受體和κ-阿片樣肽受體的配體，但其起到激動劑還是競爭拮抗劑作用目前存在爭議。[5][6]
在雄性實驗大鼠身上測試表明，口服20 mg/kg斯佩西亭後，斯佩西亭的消除半衰期為2.6 - 5小時，絕對生物利用度為20.7%[7]。
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 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 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 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 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
