SCH-442,416

SCH-442,416 structure|thumb SCH-442,416 stands out as a significant molecule in the realm of neurological pharmacology. This compound specifically targets the adenosine A2a subtype receptor, acting as an antagonist. The potency and selectivity of SCH-442,416 have implications not only for clinical treatments but also for advanced scientific investigations into the workings of the human brain.

Chemical and Biological Characteristics

SCH-442,416, by design, is a highly selective antagonist for the adenosine A2a subtype receptor^[1]. It has been utilized in its 11C radiolabelled form, which facilitates mapping the distribution of A2a receptors within the brain.

Distribution of A2a Receptors in the Brain

The A2a receptors, identified via the radiolabelled form of SCH-442,416, are prominently found in:

Striatum Nucleus accumbens Olfactory tubercle These regions play critical roles in movement, reward processing, and olfaction^[2].

Therapeutic Implications

Given the distribution of A2a receptors in the brain, there is immense interest in harnessing their potential for therapeutic applications. SCH-442,416, in particular, has shown therapeutic promise in several neurological disorders:

Depression: Studies suggest that modulation of A2a receptors might have antidepressant effects, with SCH-442,416 showing potential efficacy^[3].
Parkinson's disease: Given the prominent location of A2a receptors in movement-associated regions like the striatum, SCH-442,416 is being researched for its potential in Parkinson's disease treatment^[4].
Catalepsy: The antagonist properties of SCH-442,416 have demonstrated efficacy in reducing cataleptic behaviors in experimental models^[5].

Future Perspectives

The unique properties and potentials of SCH-442,416 necessitate further research, both for therapeutic applications and for deepening our understanding of the brain's intricate networks. As research advances, the role of adenosine A2a receptors in health and disease will undoubtedly become even clearer.

External links

Molecular Imaging and Contrast Agent Database: SCH-442,416

References

Jacobson, K. A., & Gao, Z. G. (2006). Adenosine receptors as therapeutic targets. Nature Reviews Drug Discovery, 5(3), 247-264.
Fink, J. S., Weaver, D. R., Rivkees, S. A., Peterfreund, R. A., Pollack, A. E., Adler, E. M., & Reppert, S. M. (1992). Molecular cloning of the rat A2 adenosine receptor: selective co-expression with D2 dopamine receptors in rat striatum. Brain research. Molecular brain research, 14(3), 186-195.
El Yacoubi, M., Ledent, C., Parmentier, M., Costentin, J., & Vaugeois, J. M. (2001). Adenosine A2A receptor antagonists are potential antidepressants: evidence based on pharmacology and A2A receptor knockout mice. British journal of pharmacology, 134(1), 68-77.
Pinna, A. (2014). Adenosine A2A receptor antagonists in Parkinson's disease: progress in clinical trials from the newly approved istradefylline to drugs in early development and those already discontinued. CNS drugs, 28(5), 455-474.
Ferré, S., Ciruela, F., Borycz, J., Solinas, M., Quarta, D., Antoniou, K., ... & Lluis, C. (2008). Adenosine A1-A2A receptor heteromers: new targets for caffeine in the brain. Frontiers in bioscience: a journal and virtual library, 13, 2391-2399.

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↑ Jacobson, K. A., & Gao, Z. G. (2006). Adenosine receptors as therapeutic targets. Nature Reviews Drug Discovery, 5(3), 247-264.
↑ Fink, J. S., Weaver, D. R., Rivkees, S. A., Peterfreund, R. A., Pollack, A. E., Adler, E. M., & Reppert, S. M. (1992). Molecular cloning of the rat A2 adenosine receptor: selective co-expression with D2 dopamine receptors in rat striatum. Brain research. Molecular brain research, 14(3), 186-195.
↑ El Yacoubi, M., Ledent, C., Parmentier, M., Costentin, J., & Vaugeois, J. M. (2001). Adenosine A2A receptor antagonists are potential antidepressants: evidence based on pharmacology and A2A receptor knockout mice. British journal of pharmacology, 134(1), 68-77.
↑ Pinna, A. (2014). Adenosine A2A receptor antagonists in Parkinson's disease: progress in clinical trials from the newly approved istradefylline to drugs in early development and those already discontinued. CNS drugs, 28(5), 455-474.
↑ Ferré, S., Ciruela, F., Borycz, J., Solinas, M., Quarta, D., Antoniou, K., ... & Lluis, C. (2008). Adenosine A1-A2A receptor heteromers: new targets for caffeine in the brain. Frontiers in bioscience: a journal and virtual library, 13, 2391-2399.

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[1] Jacobson, K. A., & Gao, Z. G. (2006). Adenosine receptors as therapeutic targets. Nature Reviews Drug Discovery, 5(3), 247-264.

[2] Fink, J. S., Weaver, D. R., Rivkees, S. A., Peterfreund, R. A., Pollack, A. E., Adler, E. M., & Reppert, S. M. (1992). Molecular cloning of the rat A2 adenosine receptor: selective co-expression with D2 dopamine receptors in rat striatum. Brain research. Molecular brain research, 14(3), 186-195.

[3] El Yacoubi, M., Ledent, C., Parmentier, M., Costentin, J., & Vaugeois, J. M. (2001). Adenosine A2A receptor antagonists are potential antidepressants: evidence based on pharmacology and A2A receptor knockout mice. British journal of pharmacology, 134(1), 68-77.

[4] Pinna, A. (2014). Adenosine A2A receptor antagonists in Parkinson's disease: progress in clinical trials from the newly approved istradefylline to drugs in early development and those already discontinued. CNS drugs, 28(5), 455-474.

[5] Ferré, S., Ciruela, F., Borycz, J., Solinas, M., Quarta, D., Antoniou, K., ... & Lluis, C. (2008). Adenosine A1-A2A receptor heteromers: new targets for caffeine in the brain. Frontiers in bioscience: a journal and virtual library, 13, 2391-2399.

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