LY 288513

Modify Date: 2024-01-09 16:51:25

LY 288513 Structure
LY 288513 structure
Common Name LY 288513
CAS Number 147523-65-7 Molecular Weight 436.30100
Density 1.476g/cm3 Boiling Point N/A
Molecular Formula C22H18BrN3O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of LY 288513


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].

 Names

Name LY 288513,(4S,5R)-N-(4-Bromophenyl)-3-oxo-4,5-diphenyl-1-pyrazolidinecarboxamide

 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
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