伊曲茶碱
伊曲茶碱结构式
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常用名 | 伊曲茶碱 | 英文名 | Istradefylline |
|---|---|---|---|---|
| CAS号 | 155270-99-8 | 分子量 | 384.429 | |
| 密度 | 1.2±0.1 g/cm3 | 沸点 | 601.0±65.0 °C at 760 mmHg | |
| 分子式 | C20H24N4O4 | 熔点 | N/A | |
| MSDS | 中文版 美版 | 闪点 | 317.3±34.3 °C | |
| 符号 |
GHS06 |
信号词 | Danger |
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On the role of adenosine (A)₂A receptors in cocaine-induced reward: a pharmacological and neurochemical analysis in rats.
Psychopharmacol. Ser. 232(2) , 421-35, (2015) Several studies have suggested the inhibitory control of adenosine (A)2A receptor stimulation in cocaine-induced behavioral actions.A combination of systemic or local drug injections and in vivo neurochemical analysis investigated A2A receptors in cocaine and... |
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Haloperidol promotes mTORC1-dependent phosphorylation of ribosomal protein S6 via dopamine- and cAMP-regulated phosphoprotein of 32 kDa and inhibition of protein phosphatase-1.
Neuropharmacology 72 , 197-203, (2013) The ribosomal protein S6 (rpS6) is a component of the small 40S ribosomal subunit, involved in multiple physiological functions. Here, we examined the effects produced by haloperidol, a typical antipsychotic drug, on the phosphorylation of rpS6 at Ser240/244 ... |
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Effects of the adenosine A 2A antagonist KW 6002 (istradefylline) on pimozide-induced oral tremor and striatal c-Fos expression: comparisons with the muscarinic antagonist tropicamide.
Neuroscience 163(1) , 97-108, (2009) Typical antipsychotic drugs, including haloperidol and pimozide, have been shown to produce parkinsonian motor effects such as akinesia and tremor. Furthermore, there is an antagonistic interaction between adenosine A(2A) and dopamine D(2) receptors in the ba... |
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Differential effects of presynaptic versus postsynaptic adenosine A2A receptor blockade on Δ9-tetrahydrocannabinol (THC) self-administration in squirrel monkeys.
J. Neurosci. 34(19) , 6480-4, (2014) Different doses of an adenosine A2A receptor antagonist MSX-3 [3,7-dihydro-8-[(1E)-2-(3-ethoxyphenyl)ethenyl]-7 methyl-3-[3-(phosphooxy)propyl-1-(2 propynil)-1H-purine-2,6-dione] were found previously to either decrease or increase self-administration of cann... |
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Population pharmacokinetic analysis of istradefylline in healthy subjects and in patients with Parkinson's disease.
J. Clin. Pharmacol. 51(1) , 40-52, (2011) This model-based analysis quantifies the population pharmacokinetics (PK) of orally administered istradefylline, a selective adenosine A(2A) receptor antagonist, in healthy subjects and patients with Parkinson's disease, including the estimation of covariate ... |
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Suitability of the adenosine antagonist istradefylline for the treatment of Parkinson's disease: pharmacokinetic and clinical considerations.
Expert Opin. Drug Metab. Toxicol. 9(8) , 1015-24, (2013) Recent experimental and clinical research has shown that A2A adenosine receptor antagonism can bring about an improvement in the motor behavior of patients with Parkinson's disease. Istradefylline , a xanthine derivative, has the longest half-life of all the ... |
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Functional changes in postsynaptic adenosine A(2A) receptors during early stages of a rat model of Huntington disease.
Exp. Neurol. 232(1) , 76-80, (2011) Huntington disease (HD) is a neurodegenerative disorder involving preferential loss of striatal GABAergic medium spiny neurons. Adenosine A(2A) receptors (A(2A)Rs) are present in the striatum at both presynaptic and post-synaptic levels. Blocking pre-synaptic... |
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Design and synthesis of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors.
Bioorg. Med. Chem. Lett. 22(4) , 1739-42, (2012) Monoamine oxidase-B (MAO-B) inhibitor has been used as neuroprotectants to treat the motor deficits of Parkinson's disease (PD). We designed and synthesized a class of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors. The compounds have ... |
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Positron emission tomography analysis of [11C]KW-6002 binding to human and rat adenosine A2A receptors in the brain.
Synapse 62(9) , 671-81, (2008) Adenosine A(2A) receptors are found on striatal neurones projecting to the external pallidum. KW-6002 (istradefylline) is a potent and selective antagonist for the adenosine A(2A) receptors in the CNS and acts to inhibit the excessive activity of this pathway... |
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Population pharmacokinetic-pharmacodynamic analysis of istradefylline in patients with Parkinson disease.
J. Clin. Pharmacol. 52(10) , 1468-81, (2012) This model-based analysis quantifies the population pharmacokinetic-pharmacodynamic efficacy and safety/tolerability relationships of orally administered istradefylline, a selective adenosine A(2A) receptor antagonist, in healthy participants and patients wit... |