Drug intelligence / Profile preview

11C-CGP 12177

Development stage
Preclinical
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**11C-CGP 12177** is a radiolabeled ligand used primarily as a positron emission tomography (PET) tracer for the in vivo quantification of beta-adrenoceptors (beta-adrenergic receptors), especially in cardiac tissue. It is the carbon-11 labeled form of CGP 12177, which itself is a high-affinity antagonist at beta1 and beta2 adrenoceptors and acts as a partial agonist at beta3 adrenoceptors. The compound enables noninvasive measurement of myocardial beta-adrenoceptor density and has been used to assess receptor changes in conditions such as heart failure and idiopathic cardiomyopathy[1][2][7]. Its mechanism involves binding to G-protein coupled beta-adrenoceptors on cell membranes in tissues like heart muscle, adipose tissue, and vascular smooth muscle[6]. The radiotracer is synthesized with high specific activity for intravenous injection and clinical PET imaging applications[1].

Other names
CGP 12177 hydrochlorideCGP12177 hydrochlorideCGP-12177 hydrochloride(-)-CGP-12177
02

Targets

ADRB1 (β1)ADRB2 (β2)ADRB3 (β3)

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