BL-1020

Names

[ Name ]:
BL-1020

[Synonym ]:
Butanoic acid, 4-amino-, 2-[4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]-1-piperazinyl]ethyl ester
PERPHENAZINE 4-AMINOBUTYRATE
2-{4-[3-(2-Chloro-10H-phenothiazin-10-yl)propyl]-1-piperazinyl}ethyl 4-aminobutanoate

Biological Activity

[Description]:

BL-1020 is an ester of GABA and perphenazine, fuctions as orally-active antipsychotic agent and acts as a D2 antagonist and GABA agonist; reduces dopamine activity and enhances GABAA activity, shows pro-cognitive effects and potential for the treatment of schizophrenia; displays strong dopamine and serotonin (5HT) receptor inhibition ((D2LK(iz)=0.066 nM, D(2S)Ki=0.062 nM, 5-HT2A Ki=0.21 nM). Schizophrenia Phase 2 Discontinued

[References]

References 1. Geffen Y, et al. Eur Neuropsychopharmacol. 2009 Jan;19(1):1-13. 2. Nudelman A, et al. J Med Chem. 2008 May 8;51(9):2858-62. 3. Appel L, et al. Eur Neuropsychopharmacol. 2009 Dec;19(12):841-50. 4. Geffen Y, et al. J Clin Psychiatry. 2012 Sep;73(9):e1168-74. View Related Products by Target Dopamine Receptor Schizophrenia

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
635.6±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₅H₃₄Cl₂N₄O₂S

[ Molecular Weight ]:
489.073

[ Flash Point ]:
338.2±31.5 °C

[ Exact Mass ]:
488.201263

[ LogP ]:
4.52

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.602

Related Compounds

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