Ghosh Soumita, González-Mariscal Isabel, Egan Josephine M, Moaddel Ruin
Biomedical Research Center, National Institute on Aging, National Institutes of Health, 251 Bayview Boulevard, Baltimore, MD 21224, United States.
Biomedical Research Center, National Institute on Aging, National Institutes of Health, 251 Bayview Boulevard, Baltimore, MD 21224, United States.
J Pharm Biomed Anal. 2017 Sep 10;144:154-158. doi: 10.1016/j.jpba.2016.11.003. Epub 2016 Nov 11.
Cannabinoid receptors (CBR), including CB1 and CB2 have been therapeutic targets for a number of conditions. Recently, splice variants of the CB1R have been identified in humans. The isoforms differ in their N-terminus sequence and pharmacological activity relative to the CB1R, as a result, the differentiation between the CB1 receptor and its isoform is required. As a result, a selected reaction monitoring mass spectrometry (SRM-MS) method was developed for the quantitation of CB1 and the CB1b isoform in CHO cells transduced with CB1 and CB1b. The SRM-MS protocol was assessed with isotopically labeled peptide standards and had high reproducibility of intra-day assay (CVs from 1.9 to 4.3% for CB1 and 0.5 to 5.9% for CB1b) and inter-day assay (CVs from 1.2 to 5.2% for CB1 and 1.2 to 6.1% for CB1b).
大麻素受体（CBR），包括CB1和CB2，已成为多种疾病的治疗靶点。最近，在人类中发现了CB1R的剪接变体。这些异构体在其N端序列和相对于CB1R的药理活性方面存在差异，因此，需要区分CB1受体及其异构体。为此，开发了一种选择反应监测质谱（SRM-MS）方法，用于定量转导了CB1和CB1b的CHO细胞中的CB1和CB1b异构体。使用同位素标记的肽标准品对SRM-MS方案进行了评估，其日内测定具有高重现性（CB1的CV为1.9%至4.3%，CB1b的CV为0.5%至5.9%），日间测定也具有高重现性（CB1的CV为1.2%至5.2%，CB1b的CV为1.2%至6.1%）。
