956220-35-2

Upstream product

• 130161-10-3 5-(3-Hydroxypropyl)-2-methoxybenzoic acid 
• 66411-51-6 1-[(S)-1-allylpyrrolidin-2-yl]methanamine 
• 147-85-3 L-proline 
• 114812-37-2 allyl (S)-1-allylpyrrolidine-2-carboxylate 
• 114812-43-0 (-)-(S)-1-allyl-2-pyrrolidinecarboxamide 

Downstream Products

• 713135-14-9 3-(3-(((S)-1-allylpyrrolidin-2-yl)methylcarbamoyl)-4-methoxyphenyl)propyl-4-methylbenzenesulfonate 

Relevant academic research and scientific papers

In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D2-like dopamine receptors

Benzamide derivatives as radiotracers have played an important role in diagnosing malfunction in dopaminergic neurotransmission. A variety of halogenated and two unsubstituted benzamide derivatives were synthesised and their in vitro affinities to dopaminergic, serotonergic and adrenergic receptors and their lipophilicities were determined. As references IBZM (3), raclopride (4) and FLB457 (5) were tested as well. The two iodinated compounds NAE (27) and NADE (28) displayed Ki values of 0.68 and 14 nM for the D2 receptor. The well-established radiotracers FP (1) and DMFP (2) showed affinities in the same range as did the brominated compounds NABrE (29) and NABrDE (30). The log D7.4 values of 2.91 for NAE (27) and of 2.81 for NADE (28) are in the range of those found for IBZM (3), FP (1) and DMFP (2). These facts allow to expect good properties for the two iodinated compounds NAE (27) and NADE (28) regarding in vivo imaging with SPECT.

Potential Anomalies of Dopamine D-2 Receptor: Challenges for Non-Invasive Imaging Studies by Positron Emission Tomography

We report our efforts on the development of appropriate radiopharmaceuticals for the non-invasive study of potential anomalies of dopamine D2 receptors in various brain disorders. Agonist-antagonist differences in receptor interactions necessitates that receptor radiopharmaceutical development address the question about the relative sensitivities of the neurotransmitter and radiopharmaceutical in order to detect minor alterations in receptors under various pathophysiological conditions. We are involved in the development of high affinity, selective and reversible antagonists and agonists for the in vivo study of D2 receptor. 18F-Fluorinated substituted benzamides, 18F-fallypride and 18F-desmethoxyfallypride, have now been developed as antagonists. Our efforts are now on the development of fluorinated derivatives of the selective agonist, 5-hydroxy-N-n-propyl-N-phenethyl-aminotetralin as potential radiotracers for the D2 receptors.