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CAS No.: 57982-78-2

Budipine/布地平 Catalog No. CSN10502

Synonyms: 布地平

Budipine is an uncompetitive NMDAR antagonist used as an antiparkinson agent.

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技术信息

生物活性

描述Budipine, a NMDA receptor antagonist, as a low-affinity, uncompetitive antagonist with fast kinetics and moderate voltage-dependency at the phencyclidine (PCP) binding site, comparable to that observed with amantadine, thereby counteracting an increased excitatory glutamatergic activity. The primary action of budipine is an indirect dopaminergic effect as shown by facilitation of dopamine (DA) release, inhibition of monoamine oxidase type B (MAO-B) and of DA (re) up-take and stimulation of aromatic L-amino acid decarboxylase (AADC), which in sum might be responsible for enhancing the endogenous dopaminergic activity. An additional inhibition of striatal gamma-aminobutyric acid (GABA) release by budipine may be beneficial to suppress an increased striatal GABAergic output activity^[3]. In striatal neurones, budipine blocked outward currents at +70 mV with an IC50 of 827 microM, suggesting that the binding site is less deep in the channel (delta = 0.45) than for memantine. Budipine exhibited concentration-dependent open channel blocking kinetics (kappa(on) = 0.71 x 10(4) M(-1) s(-1)) whereas the fast offset rate was concentration-independent (kappa(off) = 0.63 s(-1)). Calculation of the ratio kappa(off)/kappa(on) revealed an apparent Kd value of 88.7 microM^[4]. NMDA antagonistic action of budipine is at least partly responsible for its antiparkinsonian activity^[5]. In 6-hydroxydopamine-lesioned rats, budipine (3.13-12.5 mg/kg) and CPP (0.1-0.39 mg/kg) increased the number of contralateral rotations induced by apomorphine, whereas biperiden was not effective^[6]. Budipine and TPM (topiramate) are an effective drug combination in stopping self-sustained status epilepticus, and TPM alone was neuroprotective, despite the continuation of seizure activity^[7].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4077 mL
- 17.0387 mL
- 34.0774 mL
- 5 mM
- 0.6815 mL
- 3.4077 mL
- 6.8155 mL
- 10 mM
- 0.3408 mL
- 1.7039 mL
- 3.4077 mL

技术信息

CAS号

57982-78-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H27N

运输

蓝冰

分子量

293.45

别名

布地平

溶解度

DMSO	25.0 mg/mL (85.2 mM) warming

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