Date published: 2025-10-15

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CGS 21680 Hydrochloride (CAS 124431-80-7)

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Alternate Names:
2-p-(2-Carboxyethyl)phenethylamino-5′-N-ethylcarboxamidoadenosine hydrochloride
Application:
CGS 21680 Hydrochloride is a selective Adenosine A2A-R agonist
CAS Number:
124431-80-7
Molecular Weight:
535.98
Molecular Formula:
C23H29N7O6•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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CGS 21680 Hydrochloride is a synthetic compound that acts as a selective Adenosine A2A-R agonist. CGS 21680 Hydrochloride has found extensive use in laboratory applications to investigate muscarinic M1 receptor function both in vitro and in vivo. Functioning as a competitive antagonist of the muscarinic M1 receptor, CGS 21680 Hydrochloride binds to the receptor, thereby hindering the binding of its natural agonist, acetylcholine. This mechanism prevents receptor activation and subsequent activation of associated signaling pathways. CGS 21680 Hydrochloride exhibits a range of noteworthy biochemical and physiological effects. In vivo studies have demonstrated its potential to mitigate memory impairment, anxiety, depression, and improve motor control in models of Parkinson′s disease. Meanwhile, in vitro studies have unveiled its capacity to inhibit cell proliferation, cell migration, and cell differentiation.


CGS 21680 Hydrochloride (CAS 124431-80-7) References

  1. G protein coupling of CGS 21680 binding sites in the rat hippocampus and cortex is different from that of adenosine A1 and striatal A2A receptors.  |  Cunha, RA., et al. 1999. Naunyn Schmiedebergs Arch Pharmacol. 359: 295-302. PMID: 10344528
  2. SCH 58261 and ZM 241385 differentially prevent the motor effects of CGS 21680 in mice: evidence for a functional 'atypical' adenosine A(2A) receptor.  |  El Yacoubi, M., et al. 2000. Eur J Pharmacol. 401: 63-77. PMID: 10915839
  3. Apparent involvement of the A(2A) subtype adenosine receptor in the anti-inflammatory interactions of CGS 21680, cyclopentyladenosine, and IB-MECA with human neutrophils.  |  Visser, SS., et al. 2000. Biochem Pharmacol. 60: 993-9. PMID: 10974209
  4. Adenosine A2A receptor activation reduces proinflammatory events and decreases cell death following intracerebral hemorrhage.  |  Mayne, M., et al. 2001. Ann Neurol. 49: 727-35. PMID: 11409424
  5. The selective A2 adenosine receptor agonist CGS 21680 enhances excitatory transmitter amino acid release from the ischemic rat cerebral cortex.  |  O'Regan, MH., et al. 1992. Neurosci Lett. 138: 169-72. PMID: 1357597
  6. Binding of the prototypical adenosine A(2A) receptor agonist CGS 21680 to the cerebral cortex of adenosine A(1) and A(2A) receptor knockout mice.  |  Lopes, LV., et al. 2004. Br J Pharmacol. 141: 1006-14. PMID: 14993095
  7. Effects of adenosine and adenosine A2A receptor agonist on motor nerve conduction velocity and nerve blood flow in experimental diabetic neuropathy.  |  Kumar, S., et al. 2005. Neurol Res. 27: 60-6. PMID: 15829161
  8. Stimulation of high-affinity adenosine A2 receptors decreases the affinity of dopamine D2 receptors in rat striatal membranes.  |  Ferre, S., et al. 1991. Proc Natl Acad Sci U S A. 88: 7238-41. PMID: 1678519
  9. The adenosine A2A receptor agonist CGS 21680 fails to ameliorate the course of dextran sulphate-induced colitis in mice.  |  Selmeczy, Z., et al. 2007. Inflamm Res. 56: 204-9. PMID: 17588136
  10. Intra-accumbens injections of the adenosine A2A agonist CGS 21680 affect effort-related choice behavior in rats.  |  Font, L., et al. 2008. Psychopharmacology (Berl). 199: 515-26. PMID: 18491078
  11. Excitatory effect of the A2A adenosine receptor agonist CGS-21680 on spontaneous and K+-evoked acetylcholine release at the mouse neuromuscular junction.  |  Palma, AG., et al. 2011. Neuroscience. 172: 164-76. PMID: 20971164
  12. CGS 21680, an agonist of the adenosine (A2A) receptor, reduces progression of murine type II collagen-induced arthritis.  |  Mazzon, E., et al. 2011. J Rheumatol. 38: 2119-29. PMID: 21765105
  13. The adenosine A2A receptor agonist CGS 21680 decreases ethanol self-administration in both non-dependent and dependent animals.  |  Houchi, H., et al. 2013. Addict Biol. 18: 812-25. PMID: 23301633
  14. The adenosine A(2A) receptor agonist CGS 21680 alleviates auditory sensorimotor gating deficits and increases in accumbal CREB in rats neonatally treated with quinpirole.  |  Brown, RW., et al. 2020. Psychopharmacology (Berl). 237: 3519-3527. PMID: 32772144

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

CGS 21680 Hydrochloride, 10 mg

sc-211062
10 mg
$286.00

CGS 21680 Hydrochloride, 50 mg

sc-211062A
50 mg
$1024.00