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Carbidopa

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Chemical Structure| 28860-95-9 同义名 : (S)-(-)-Carbidopa
CAS号 : 28860-95-9
货号 : A587591
分子式 : C10H14N2O4
纯度 : 98%
分子量 : 226.229
MDL号 : MFCD00069231
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(39.78 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

4% DMSO+30% PEG 300+2% Tween 80+water 1 mg/mL

生物活性
靶点

  • decarboxylase

    aromatic-L-amino-acid decarboxylase, IC50:29 μM
描述 Aromatic L-amino acid decarboxylase (AADC) is the final enzyme in the biosynthesis of the monoamine neurotransmitters serotonin and dopamine, and dopamine is the precursor for norepinephrine and epinephrine[3]. Carbidopa (CD), a competitive inhibitor of AADC that doesn’t cross the blood-brain barrier, is routinely administered with levodopa (LD) to patients with Parkinson disease (PD) to reduce the peripheral decarboxylation of LD to dopamine[4]. On exposure to other human tumor lines, CD was lethal only to NCI-H146 and NCI-H209 small cell lung carcinoma (SCLC) lines (IC50 = 12 ± 1 μM and 22 ± 5 μM, respectively). CD (100 μM) decreased growth of SK-N-SH neuroblastoma and A204 rhabdomyosarcoma cells[5]. For all patients with cerebrospinal fluid (CSF), AUC (area under the curve) serum CD significantly correlated with percent-labeled CSF HVA (R = 0.786, p = 0.02). In addition, a significantly greater percent-labeled CSF HVA was present in “rapid” as compared to “slow” CD absorbers (Patients were divided into “slow” absorbers (those unable to attain a serum CD level of at least 300 ng/ml within 3 hours after CD administration) and those with more “rapid” absorption (patients obtaining a level of 300 ng/ml or greater within the first 3 hours))[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01766258 Parkinson's Disease Phase 2 Completed - -
NCT01663935 Albinism Ocul... 展开 >>ocutaneous Albinism 收起 << Phase 2 Recruiting October 2017 United States, Wisconsin ... 展开 >> University of Wisconsin Recruiting Madison, Wisconsin, United States, 53705 Contact: Angie Wealti    608-265-7557    Angie Wealti    Principal Investigator: Michael C Struck, MD 收起 <<
NCT01468012 Cocaine Dependence Phase 2 Phase 3 Completed - United States, New York ... 展开 >> STARS New York, New York, United States, 10032 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.42mL

0.88mL

0.44mL

22.10mL

4.42mL

2.21mL

44.20mL

8.84mL

4.42mL
参考文献

[1]Orlefors H, Sundin A, et al. Carbidopa pretreatment improves image interpretation and visualisation of carcinoid tumours with 11C-5-hydroxytryptophan positron emission tomography. Eur J Nucl Med Mol Imaging. 2006 Jan;33(1):60-5.

[2]Durso R, Evans JE, et al. Variable absorption of carbidopa affects both peripheral and central levodopa metabolism. J Clin Pharmacol. 2000 Aug;40(8):854-60.

[3]Wassenberg T, Molero-Luis M, Jeltsch K, et al. Consensus guideline for the diagnosis and treatment of aromatic l-amino acid decarboxylase (AADC) deficiency. Orphanet J Rare Dis. 2017;12(1):12

[4]Durso R, Evans JE, Josephs E, et al. Variable absorption of carbidopa affects both peripheral and central levodopa metabolism. J Clin Pharmacol. 2000;40(8):854‐860

[5]Gilbert JA, Frederick LM, Ames MM. The aromatic-L-amino acid decarboxylase inhibitor carbidopa is selectively cytotoxic to human pulmonary carcinoid and small cell lung carcinoma cells. Clin Cancer Res. 2000;6(11):4365‐4372