CGS-21680

CGS-21680

CGS-21680 is a pivotal molecule within neuropharmacology, specifically as an agonist for the adenosine A2A subtype receptor. While its current application remains predominantly in research, it offers potential insights into the deeper mechanisms of neuronal transmission.

Chemical Characteristics

• Molecular Form: CGS-21680 is typically encountered as an organic hydrochloride salt.
• Molecular Weight: It has a molecular weight of 536.0 g/M.

Solubility: Up to 3.4 mg/mL in DMSO (Dimethyl sulfoxide). Up to 20 mg/mL in 45% (w/v) aqueous 2-hydroxypropyl-β-cyclodextrin.

Research Implications

The prime interest in CGS-21680 emanates from its role as a high-affinity, subtype-specific analogue for adenosine, a naturally occurring neurotransmitter. Such analogues help researchers to elucidate the role of adenosine in various physiological and neurological processes.

• Neuronal Transmission: By mimicking the effects of adenosine in a targeted manner, CGS-21680 provides insights into how adenosine receptors influence neuronal transmission.
• Respiratory Rhythmicity: The drug has been instrumental in respiratory studies, especially regarding the pre-Bötzinger complex, a neural structure believed to play a role in rhythm generation. Specifically, A2A receptors are postulated to influence this rhythm generation.

Therapeutic Potential

While CGS-21680 serves as a valuable research tool, it has not yet garnered approval for therapeutic use. However, given its role in elucidating the functions of adenosine receptors, there's potential for its analogues or derivatives to contribute to therapeutic strategies in the future.

Limitations and Considerations

As with all research compounds, users of CGS-21680 must be aware of its specificities, including its solubility parameters, and should use it judiciously, understanding that its primary role is in experimental applications and not therapeutic interventions.

See also

• Adenosine receptor

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References

Stone, T. W., & Ceruti, S. (2007). Adenosine receptors and neurological disease: Neuroprotection and neurodegeneration. Handbook of Experimental Pharmacology, (193), 535-587. Herlenius, E., & Lagercrantz, H. (2004). Neurotransmitters and neuromodulators during early human development. Early human development, 79(1), 21-37.

• Mayer CA, Haxhiu MA, Martin RJ, Wilson CG,

 Adenosine A2A receptors mediate GABAergic inhibition of respiration in immature rats, 
 J Appl Physiol, 
 2006,
 Vol. 100(Issue: 1),
 pp. 91–97,
 DOI: 10.1152/japplphysiol.00459.2005,
 PMID: 16141383,

• Xie S, Shafer G, Wilson CG, Martin HB,

 In vitro adenosine detection with a diamond-based sensor, 
 Dia Rel Mater, 
 2006,
 Vol. 15(Issue: 2-3),
 pp. 225–228,
 DOI: 10.1016/j.diamond.2005.08.018,