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/ 脱羧酶 / Carbidopa/卡比多巴

Carbidopa/卡比多巴 {[allProObj[0].p_purity_real_show]}

货号：A587591 同义名： (S)-(-)-Carbidopa

Carbidopa是一种芳香 L-氨基酸脱羧酶抑制剂，IC50 为 29 ± 2 μM。

Carbidopa/卡比多巴 化学结构 CAS号：28860-95-9
Carbidopa/卡比多巴 化学结构
CAS号：28860-95-9
Carbidopa/卡比多巴 3D分子结构
CAS号：28860-95-9
Carbidopa/卡比多巴 化学结构 CAS号：28860-95-9
Carbidopa/卡比多巴 3D分子结构 CAS号：28860-95-9
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Carbidopa/卡比多巴 纯度/质量文件 产品仅供科研

货号：A587591 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 decarboxylase ↓ 其他靶点 纯度
Eflornithine HCl hydrate ✔ 98%
Methyldopa ✔ 98%
Benserazide HCI ✔ 98%
Carbidopa +++

aromatic-L-amino-acid decarboxylase, IC50: 29 μM

 		99% (LCMS)
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Carbidopa/卡比多巴 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].

Carbidopa/卡比多巴 细胞实验

Cell Line
Concentration Treated Time Description References
Ruminococcus gnavus 1.5 mM 24 hours Evaluate the inhibitory effect of Carbidopa on PEA production Gut Microbes. 2022 Jan-Dec;14(1):2128605.
Enterococcus faecalis 1.5 mM 24 hours Evaluate the inhibitory effect of Carbidopa on PEA production Gut Microbes. 2022 Jan-Dec;14(1):2128605.

Carbidopa/卡比多巴 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Female MF1 mice Mouse marble-burying behavior model Intraperitoneal injection 9 mg/kg Single dose Carbidopa alone reduced marble burying but did not affect runway activity. When co-administered with 5-HTP, it significantly reduced both marble burying and runway activity. Br J Pharmacol. 1991 Sep;104(1):105-12
Mice COMT gene-disrupted mice and S-COMT-deficient mice Oral 30 mg/kg Single dose To investigate the pharmacokinetic effects of carbidopa co-administered with L-DOPA in COMT gene-disrupted and S-COMT-deficient mice. Results showed that carbidopa co-administered with L-DOPA significantly increased L-DOPA levels in plasma and peripheral tissues of COMT-KO mice, while significantly decreasing 3-O-methyldopa levels in S-COMT-deficient mice. Br J Pharmacol. 2009 Dec;158(8):1884-94
Mice Dopamine-deficient mouse model Intraperitoneal injection 12.5 or 25 mg/kg Single administration Carbidopa, when co-administered with L-DOPA, elevates brain dopamine concentrations and induces stereotypy. Proc Natl Acad Sci U S A. 1999 Oct 12;96(21):12138-43
Mice Dopamine-deficient (DD) mice Intraperitoneal injection 10 mg/kg Single administration Carbidopa was administered with L-DOPA to inhibit peripheral L-aromatic amino acid decarboxylase activity, thereby increasing L-DOPA delivery to the brain and elevating brain dopamine levels. When striatal DA levels exceeded 50% of WT levels, a transition from hyperlocomotion to intense, focused stereotypy was observed in DD mice. Proc Natl Acad Sci U S A. 2001 Aug 28;98(18):10451-6
Nude mice PNEC tumor xenograft model Intraperitoneal injection 100 mg/kg Once daily for 30 days To evaluate the inhibitory effect of Carbidopa combined with other drugs on PNEC tumor growth, results showed a significant 40% reduction in tumor growth Proc Natl Acad Sci U S A. 2006 Aug 15;103(33):12505-10
Mice and rats 8-OH-DPAT-induced hypothermia model Intraperitoneal injection 25 mg/kg Administered 60 min before 5-HTP In mice, carbidopa combined with 5-HTP virtually abolished 8-OH-DPAT-induced hypothermia (93% attenuation); no significant effect was observed in rats Br J Pharmacol. 1991 Aug;103(4):1857-64
Rats and mice Reserpine-induced Parkinson's disease model Intraperitoneal injection 50 mg/kg Administered 1 hour before Carbidopa combined with L-DOPA reversed reserpine-induced akinesia and hypothermia, and increased striatal dopamine levels Br J Pharmacol. 1999 Apr;126(7):1667-73

Carbidopa/卡比多巴 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 <<

Carbidopa/卡比多巴 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

Carbidopa/卡比多巴 实验方案

计算器
存储液制备 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

Carbidopa/卡比多巴 技术信息

CAS号28860-95-9
分子式C10H14N2O4
分子量 226.23
SMILES Code O=C([C@@](NN)(CC1=CC=C(C(O)=C1)O)C)O
MDL No. MFCD00069231
别名 (S)-(-)-Carbidopa
运输蓝冰
InChI Key TZFNLOMSOLWIDK-JTQLQIEISA-N
Pubchem ID 34359
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Carbidopa | 28860-95-9 | (S)-(-)-Carbidopa | Aryl Hydrocarbon Receptor | Decarboxylase Inhibitor | Immunology/Inflammation | Aryl Hydrocarbon Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Carbidopa/卡比多巴 纯度/质量文件 | Carbidopa/卡比多巴 亚型比较 | Carbidopa/卡比多巴 生物活性 | Carbidopa/卡比多巴 临床数据 | Carbidopa/卡比多巴 参考文献 | Carbidopa/卡比多巴 实验方案 | Carbidopa/卡比多巴 技术信息

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