Carbidopa Monohydrate

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Chemical Structure| 38821-49-7 同义名 : 卡比多巴水合物 ;Carbidopa(hydrate);S(-)-Carbidopa;(S)-(-)-Carbidopa monohydrate
CAS号 : 38821-49-7
货号 : A788203
分子式 : C10H16N2O5
纯度 : 97%
分子量 : 244.244
MDL号 : MFCD00889211
存储条件:

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
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[1]. Carbidopa monohydrate is the monohydrate form of Carbidopa. 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[2]. 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[3]. 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))[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.09mL

0.82mL

0.41mL

20.47mL

4.09mL

2.05mL

40.94mL

8.19mL

4.09mL

参考文献

[1]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

[2]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

[3]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