Caffeine Citrate

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Cat Number

API69227

CAS Number

69-22-7

For research use only. We do not supply to patients.

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Product Detail Description Scientific Support Customer Q&A

CAS Number

69-22-7

Storage

2-8℃

Synonyms

1,3,7-TRIMETHYL-2,6-DIOXOPURINE CITRATE

Molecular Formula

C14H18N4O9

Molecular Weight

386.31

Smiles

CN1C=NC2=C1C(=O)N(C(=O)N2C)C.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

Appearance

White to off-white solid

Melting Point

159-161℃

General Description

Caffeine Citrate is a salt formed between caffeine (1,3,7-trimethylxanthine), a naturally occurring methylxanthine alkaloid, and citric acid. The citrate salt form provides improved aqueous solubility and stability compared to anhydrous caffeine, making it suitable for pharmaceutical research applications.

Mechanism of Action

Caffeine acts as a competitive non-selective antagonist at adenosine A1 and A2A receptors, blocking adenosine's inhibitory effects on neuronal activity. It also inhibits phosphodiesterase enzymes at higher concentrations, increasing intracellular cAMP levels and promoting adrenergic neurotransmission.

Application

Indicated for the treatment of apnea of prematurity in neonates. Caffeine Citrate is a methylxanthine respiratory stimulant that improves central respiratory drive, reduces episodes of apnea and bradycardia in premature infants, and provides enhanced aqueous solubility for accurate dosing in neonatal care.

Caffeine citrate significantly inhibited sepsis-associated encephalopathy-induced neuronal apoptosis and astrocytic activation in rat cerebral cortex, decreased reactive oxygen species generation, and elevated mitochondrial membrane potential levels. In lipopolysaccharide and interferon-gamma-stimulated primary astrocytes, caffeine citrate reduced ROS and MMP levels and inhibited mitochondrial complex enzyme activities. Caffeine citrate promoted UCP2 expression in astrocytes while inhibiting NLRP3 inflammasome activation and reducing IL-1β and IL-18 production both in vivo and in vitro.

References

Hu J, et al. Caffeine citrate protects against sepsis-associated encephalopathy and inhibits the UCP2/NLRP3 axis in astrocytes. Journal of Interferon & Cytokine Research, 2022, 42(6): 267-278.

Why is Caffeine Citrate preferred over anhydrous caffeine in neonatal therapy?

Caffeine Citrate offers significantly higher aqueous solubility and greater solution stability compared to anhydrous caffeine, making it the preferred form for precise neonatal dosing.