PD 135158

Names

[ Name ]:
PD 135158

[Synonym ]:
car011

Biological Activity

[Description]:

PD 135158 (CAM 1028) is a selective CCKB receptor antagonist with an IC50 of 2.8 nM against mouse cortex CCKB. PD 135158 shows anxiolytic activity[1].

[Related Catalog]:

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

Research Areas >> Neurological Disease

[Target]

CCKBR:2.8 nM (IC50)

CCKAR:1232 nM (IC50)

[In Vivo]

PD 135158 (CAM 1028; 0.001-0.1 mg/kg; s.c.; once) 增强大鼠的潜在抑制作用，显示出抗精神病潜能[2]。 Animal Model: Male Sprague-Dawley rats, conditioned suppression of drinking procedure model[2] Dosage: 0.001, 0. 01, and 0.1 mg/kg Administration: 0.2 mL/kg SC 30 min before prexposure and conditioning Result: Elicited a clear latent inhibition effect under conditions that did not lead to latent inhibition in control rats.

[References]

[1]. Hughes J, et al. Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc Natl Acad Sci U S A. 1990 Sep;87(17):6728-32.

[2]. Gracey DJ, et al. PD-135,158, a cholecystokinin(B) antagonist, enhances latent inhibition in the rat. Pharmacol Biochem Behav. 2000 Mar;65(3):459-63.

Chemical & Physical Properties

[ Boiling Point ]:
860.3ºC at 760 mmHg

[ Molecular Formula ]:
C₄₂H₆₁N₅O₁₁

[ Molecular Weight ]:
811.96

[ Flash Point ]:
474.1ºC

[ Exact Mass ]:
616.32600

[ PSA ]:
149.62000

[ LogP ]:
6.42130

[ Vapour Pressure ]:
1.51E-31mmHg at 25°C

PD 135158

Names

Biological Activity

Chemical & Physical Properties

Related Compounds