LY 288513

Names

[ Name ]:
LY 288513

Biological Activity

[Description]:

LY288513, a selective non-peptide CCK-B receptor antagonist with an IC50 value of 16 nM. LY288513 possesses both anxiolytic and antipsychotic potential[1][2][3].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Cholecystokinin Receptor

Research Areas >> Neurological Disease

[Target]

IC50: 16 nM (CCK-B receptor)[1]

[In Vitro]

LY288513 (10 nM; 2 days) suppresses the effects of CCK-8 on CD4+ T cell subset-specific transcription factors[2]. RT-PCR[2] Cell Line: CD4+ T cells Concentration: 10 nM Incubation Time: 2 days Result: Suppressed the effects of CCK-8 on CD4+ T cell subset-specific transcription factors.

[In Vivo]

LY288513 (3, 10 mg/kg, i.p.; 10, 30 mg/kg, p.o.) produces an anxiolytic-like action[3]. LY288513 (1000 mg/kg, p.o.) potentiates the effects of a CNS depressant, slightly lowered body temperature, and had modest sedative effects only at the highest dose examined[3]. Animal Model: Male CD-l mice[3] Dosage: 3, 10 mg/kg; 10, 30 mg/kg Administration: I.p.; p.o. Result: Displayed anxiolytic-like effects in the elevated plusmaze.

[References]

[1]. Rasmussen K. CCK, schizophrenia, and anxiety. CCK-B antagonists inhibit the activity of brain dopamine neurons. Ann N Y Acad Sci. 1994 Mar 23;713:300-11.

[2]. Zhang JG, et al. Cholecystokinin octapeptide regulates the differentiation and effector cytokine production of CD4(+) T cells in vitro. Int Immunopharmacol. 2014;20(2):307-315.

[3]. Helton DR, et al. Central nervous system characterization of the new cholecystokininB antagonist LY288513. Pharmacol Biochem Behav. 1996 Mar;53(3):493-502.

Chemical & Physical Properties

[ Density]:
1.476g/cm3

[ Molecular Formula ]:
C₂₂H₁₈BrN₃O₂

[ Molecular Weight ]:
436.30100

[ Exact Mass ]:
435.05800

[ PSA ]:
61.44000

[ LogP ]:
5.19260

[ Index of Refraction ]:
1.676

Related Compounds

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