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Piclozotan

Catalog No. T28414   CAS 182415-09-4
Synonyms: SUN-N-4057, SUN4057, SUNN-4057, SUN-4057, SUNN4057

Piclozotan (anhydrous), a 5-HT1A receptor agonist, demonstrated significant neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model, ameliorating motor complications in patients with advanced Parkinson's disease.

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Piclozotan Chemical Structure
Piclozotan, CAS 182415-09-4
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1 mg 6-8weeks $ 210.00
5 mg 6-8weeks $ 530.00
10 mg 6-8weeks $ 800.00
25 mg 6-8weeks $ 1,551.00
50 mg 6-8weeks $ 1,980.00
100 mg 6-8weeks $ 2,500.00
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Biological Description
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Description Piclozotan (anhydrous), a 5-HT1A receptor agonist, demonstrated significant neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model, ameliorating motor complications in patients with advanced Parkinson's disease.
In vivo Piclozotan (SUN N4057) (0.018 and 0.036 mg/kg/h; continuous subcutaneous infusion; 3 to 4 weeks; Parkinsonian rats) significantly lengthened the duration of rotational behavior by 26% and attenuated the increase in striatal levodopa-derived extracellular dopamine levels compared with the control group. Piclozotan (0.018 and 0.036 mg/kg/h, plasma concentrations 5.3±0.7 and 14.3±2.9 ng/ml) reduced levodopa-induced forelimb hyperkinesia by 55% and 69%, respectively, at 1h relative to the control.[1]
Synonyms SUN-N-4057, SUN4057, SUNN-4057, SUN-4057, SUNN4057
Molecular Weight 409.91
Formula C23H24ClN3O2
CAS No. 182415-09-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Tani Y, et al Effects of piclozotan (SUN N4057), a partial serotonin 1A receptor agonist, on motor complications induced by repeated administration of levodopa in parkinsonian rats. Eur J Pharmacol. 2010;649(1-3):218-223. 2. Mondick JT, et al. Population pharmacokinetics of the selective serotonin 5-HT1A receptor partial agonist piclozotan. Am J Ther. 2009;16(2):106-115. 3. Kamei K, et al. Synthesis, SAR studies, and evaluation of 1,4-benzoxazepine derivatives as selective 5-HT1A receptor agonists with neuroprotective effect: Discovery of Piclozotan. Bioorg Med Chem. 2006;14(6):1978-1992. 4. Ferro JM, et al. Other neuroprotective therapies on trial in acute stroke. Cerebrovasc Dis. 2006;21 Suppl 2:127-130.

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Keywords

Piclozotan 182415-09-4 GPCR/G Protein Neuroscience 5-HT Receptor SUN-N-4057 SUN-N4057 SUN 4057 SUN4057 SUNN 4057 SUN-N 4057 SUNN-4057 SUN-4057 SUNN4057 inhibitor inhibit

 

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