130325-35-8

130325-35-8 structure

Name: PD 135158
Chemical Name: 1-deoxy-1-(methylamino)
CAS Number: 130325-35-8
Molecular Formula: C₄₂H₆₁N₅O₁₁
Molecular Weight: 811.96
Catalog: Signaling Pathways GPCR/G Protein Cholecystokinin Receptor
Create Date: 2017-01-10 15:56:06
Modify Date: 2024-01-28 06:59:21
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].

Name	1-deoxy-1-(methylamino)
Synonyms	car011

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.