1187651-71-3

Upstream product

• 81147-92-4 esmolol 
• 107-15-3 ethylenediamine 

Relevant academic research and scientific papers

Synthesis and In Vivo Evaluation of a Kit-Type 99mTc-labeled N-(2-Aminoethyl)-3-(4-(2-hydroxy-3-(isopropylaminopropoxy)phenyl)propanamide as a Selective β1-Adrenoceptor-binding SPECT Radiotracer

To develop a novel β1-adrenoceptor selective radiotracer, 99mTc-labeld N-(2-aminoethyl)-3-(4-(2-hydroxy-3-(isopropylaminopropoxy)phenyl)propanamide ([99mTc]1) was prepared by incorporating [99mTcO4]? into the precursor 3. Radiotracer [99mTc]1 was optimized in several reaction conditions for kit-type preparation of 99mTc-radiopharmaceuticals. The radiochemical yield was around 95% (non-decay corrected) within 30 s labeling time and radiochemical purity showed over 98%. In image studies, [99mTc]1 provided a good heart accumulation, whereas liver and lung uptakes showed relatively low at initial time. Furthermore, [99mTc]1 images at 25 min post-injection provided a clearly visible cardiac image with high contrast. To confirm the β1-adrenoceptor-binding specificity of [99mTc]1, a blocking experiment was performed. In vivo blocking with excess esmolol (18 mg/kg) or atenolol (2 mg/kg) resulted in significantly reduced radioactivity uptake in the heart around 92 and 76%, respectively. The results suggested that [99mTc]1 might be of worth applying to the assessment of β1-adrenoceptor expression in the heart diseases.

IMAGE-GUIDED THERAPY OF MYOCARDIAL DISEASE: COMPOSITION, MANUFACTURING AND APPLICATIONS

Compositions and methods for imaging and for chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns agents comprising a targeting moeity comprising a beta-adrenergic receptor targeting compound conjugated or embedded with ethylenediamine. The present invention also concerns methods of application of such agents for imaging and treatment of cardiovascular diseases, and kits for preparing a radiolabeled therapeutic or diagnostic agent.