PD 135158

Modify Date: 2024-01-28 06:59:21

PD 135158 Structure
PD 135158 structure
Common Name PD 135158
CAS Number 130325-35-8 Molecular Weight 811.96
Density N/A Boiling Point 860.3ºC at 760 mmHg
Molecular Formula C42H61N5O11 Melting Point N/A
MSDS N/A Flash Point 474.1ºC

 Use of PD 135158


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].

 Names

Name 1-deoxy-1-(methylamino)
Synonym More Synonyms

 PD 135158 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
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

 Synonyms

car011
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