Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with K_i of 2.2 nM in experimental models of Parkinsons disease.

Solid

Ki: 2.2 nM (adenosine A2A receptor)

Istradefylline has 70-fold greater affinity for the A2AR than the A1 receptor with K_i of 2.2 nM versus 150 nM. Istradefylline causes concentration-dependent abolition of bFGF induction of astrogliosis in primary rat striatal astrocytes. Istradefylline binds to A1 receptor, A2A receptor, and A3 receptor in human with K_is of >287 nM, 9.12 nM, and >681 nM, respectively, 50.9 nM and 1.57 nM for A1 receptor and A2A receptor in rat, 105.02 nM and 1.87 nM for A1 receptor and A2A receptor in mouse, respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Istradefylline (3.3 mg/kg, i.p.) treatment before a single dose of MPTP attenuates the partial dopamine and DOPAC depletions measured in striata 1 week later. Istradefylline reverses CGS21680-induced and reserpine-induced catalepsy with an ED₅₀ of 0.05 mg/kg and 0.26 mg/kg, respectively. Istradefylline is over 10 times as potent in these models compared to other adenosine antagonists and dopamine agonist drugs. Istradefylline combined with L-dopa cuases potent effects on haloperidol-induced and reserpine-induced catalepsy. Istradefylline (10 mg/kg, p.o.) results an increase in locomotor activity to approximately twice that of control and improves motor disability in MPTP-treated common marmosets. Istradefylline (10 mg/kg, p.o.) in combination with SKF80723, quinpirole, or L-DOPA produces a significant additive effect on locomotor activity and improvement of motor disability but not dysK_inesia.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature or refrigerated transportation.

• [1]. Chen JF, et al. Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinsons disease. J Neurosci. 2001 May 15;21(10):RC143.  [Information]

  [2]. Shiozaki S, et al. Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP. Psychopharmacology (Berl). 1999 Nov;147(1):90-5.  [Information]

  [3]. Kanda T, et al. Combined use of the adenosine A(2A) antagonist KW-6002 with L-DOPA or with selective D1 or D2 dopamine agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys. Exp Neurol. 2000 Apr;162(2):321-7.  [Information]

  [4]. Brambilla R, et al. Blockade of A2A adenosine receptors prevents basic fibroblast growth factor-induced reactive astrogliosis in rat striatal primary astrocytes. Glia. 2003 Aug;43(2):190-4.  [Information]

  [5]. Mihara T, et al. Pharmacological characterization of a novel, potent adenosine A1 and A2A receptor dual antagonist, 5-[5-amino-3-(4-fluorophenyl)pyrazin-2-yl]-1-isopropylpyridine-2(1H)-one (ASP5854), in models of Parkinsons disease and cognition. J Pharm  [Information]

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。