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Chemical Structure| 120225-54-9 Chemical Structure| 120225-54-9

Structure of CGS 21680
CAS No.: 120225-54-9

Chemical Structure| 120225-54-9

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CGS 21680 is a selective Adenosine A2A Receptor agonist with a Ki value of 27 nM.

Synonyms: CGS 21680

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Product Details of CGS 21680

CAS No. :120225-54-9
Formula : C23H29N7O6
M.W : 499.52
SMILES Code : CCNC([C@@H]1[C@@H](O)[C@@H](O)[C@H](N2C=NC3=C2N=C(NCCC4=CC=C(CCC(O)=O)C=C4)N=C3N)O1)=O
Synonyms :
CGS 21680
MDL No. :MFCD00078573

Safety of CGS 21680

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of CGS 21680

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CA1 pyramidal neurons 30 nM 40 min To evaluate the influence of adenosine A2A receptors on NMDA receptor activity in CA1 hippocampal neurons. Results showed that CGS 21680 significantly enhanced NMDA receptor-mediated currents through A2A receptor activation, an effect blocked by the A2A receptor antagonist SCH58261 and the PKA inhibitor H-89. PMC6240125
Human neutrophils 0.01 – 1 μM 10 min Investigated the effects of CGS 21680 on reactive oxidant production, elastase release, cytosolic Ca2+ fluxes, and intracellular cyclic AMP concentrations in FMLP-activated human neutrophils. Results showed CGS 21680 accelerated Ca2+ resequestration and inhibited oxidant production and elastase release. PMC1572119
Rat cerebral cortex synaptosomes 0.01 nM 6 min To investigate the effect of CGS 21680 on K+-evoked endogenous glutamate overflow, results showed that 0.01 nM CGS 21680 significantly enhanced the overflow, and this effect was blocked by 0.1 μM SCH58261. PMC1573357
Rat cerebral cortex synaptosomes 0.01 nM 6 min To investigate the effect of CGS 21680 on Ca2+-dependent K+-evoked [3H]-D-aspartate overflow, results showed that 0.01 nM CGS 21680 significantly enhanced the overflow (47.69±6.2%), and this effect was completely blocked by the A2A receptor antagonist SCH58261. PMC1573357
Peritoneal macrophages 5 μM 24 h To evaluate the effect of CGS-21680 on TNF-α and MCP-1 secretion in peritoneal macrophages exposed to LPS plus oxygen. Results showed that CGS-21680 significantly reduced TNF-α and MCP-1 secretion. PMC3707379
MH-S cells 5 μM 24 h To evaluate the effect of CGS-21680 on TNF-α and MIP-2 secretion in MH-S cells exposed to LPS plus oxygen. Results showed that CGS-21680 significantly reduced TNF-α and MIP-2 secretion. PMC3707379

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Acute heart failure model Intravenous infusion 0.1, 0.3 and 1.0 mg/kg/min 15 minutes To assess the effects of CGS 21680 on cardiac output and vascular resistance in rats with acute heart failure. Results showed that the highest dose of CGS 21680 significantly reduced blood pressure, arterial resistance, and left ventricular end-diastolic pressure, while significantly increasing cardiac output (28%) and heart rate (10%). Additionally, the highest dose of CGS 21680 significantly reduced mean circulatory filling pressure (9%) and venous resistance (62%). PMC1565321
Adult male CF1 mice Memory impairment model Intraperitoneal or intracerebroventricular injection 0.1–0.5 mg/kg (i.p.) or 50 nM (i.c.v.) Single administration, 30 min before training Activation of A2A receptors was sufficient to trigger short-term memory impairment in three behavioral tests, and this effect was blocked by SCH 58261 (A2A receptor antagonist). PMC4523339
Mice LPS-induced lung injury model Intraperitoneal injection 125 μg/mouse Administered at 12, 36, and 60 hours after initiation of oxygen exposure To evaluate the effect of CGS-21680 on lung injury in mice exposed to LPS plus oxygen. Results showed that CGS-21680 significantly reduced histologic lung injury, BAL protein, and alveolar cell counts. PMC3707379
Mice STZ-induced type 1 diabetic mouse model Femoral vein injection 0.5 mg/kg Single injection Evaluate the effect of CGS 21680 on coronary blood flow PMC4729563
Adult female Sprague-Dawley rats OVX female rats Local infusion into the MnPO 24 Nm Single injection, recorded for 8 hours To test whether E2 attenuates A2A receptor actions in the MnPO, results showed E2 significantly attenuated CGS-21680-induced increase in NREM sleep PMC8919205

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