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Budipine

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Chemical Structure| 57982-78-2 同义名 : -
CAS号 : 57982-78-2
货号 : A187972
分子式 : C21H27N
纯度 : 99%+
分子量 : 293.45
MDL号 : MFCD00866585
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(85.19 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：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.41mL

0.68mL

0.34mL

17.04mL

3.41mL

1.70mL

34.08mL

6.82mL

3.41mL
参考文献

[1]Reichmann H. Budipine in Parkinson's tremor. J Neurol Sci. 2006 Oct 25;248(1-2):53-5.

[2]Jellinger K, Bliesath H. Adjuvant treatment of Parksinson's disease with budipine: a double-blind trial versus placebo. J Neurol. 1987 Jun;234(5):280-2.

[3]Eltze M. Multiple mechanisms of action: the pharmacological profile of budipine. J Neural Transm Suppl. 1999;56:83-105

[4]Parsons CG, Hartmann S, Spielmanns P. Budipine is a low affinity, N-methyl-D-aspartate receptor antagonist: patch clamp studies in cultured striatal, hippocampal, cortical and superior colliculus neurones. Neuropharmacology. 1998 Jun;37(6):719-27

[5]Klockgether T, Jacobsen P, Löschmann PA, Turski L. The antiparkinsonian agent budipine is an N-methyl-D-aspartate antagonist. J Neural Transm Park Dis Dement Sect. 1993;5(2):101-6

[6]Klockgether T, Wüllner U, Steinbach JP, Petersen V, Turski L, Löschmann PA. Effects of the antiparkinsonian drug budipine on central neurotransmitter systems. Eur J Pharmacol. 1996 Apr 22;301(1-3):67-73

[7]Fisher A, Wang X, Cock HR, Thom M, Patsalos PN, Walker MC. Synergism between topiramate and budipine in refractory status epilepticus in the rat. Epilepsia. 2004 Nov;45(11):1300-7