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Caffeine is a central nervous system stimulant that binds adenosine receptors. Adenosine receptors are a class of GPCRs involved in heart and blood flow, inflammation, and neurotransmission. These receptors are potential drug targets for tissue damage, brain, kidney and liver injury, epilepsy, Parkinson's disease, and Huntington's disease.

We offer both agonist and antagonist radioligands for autoradiographic visualization or performing saturation and competition assays to determine receptor expression levels (B_max), dissociation constants (K_d), association and dissociation rates (k_on and k_off), and inhibitor constants (K_i) for a variety of receptors. We develop our radioligands to the highest specific activity possible and provide high purity resulting in low non-specific binding products. Each of our ultra-pure radioligands is fully characterized for pharmacological action and validated in receptor binding assays.

Radiolabeled ligands remain the most sensitive method for probing receptor binding biology; yielding unprecedented sensitivity gives results that technicians and scientists can trust. For over 50 years, PerkinElmer has been a leading supplier of New Englａnd Nuclear (NEN) radiochemicals, liquid scintillation cocktails, vials and nuclear counting detection instruments.

References for NEC412:

1. Eberhard Schrader, G?tz Klaunick, Ute Jorritsma, Hartmud Neurath, Karen I Hirsch-Ernst, Georg F Kahl, Heidi Foth, High-performance liquid chromatographic method for simultaneous determination of [1-methyl-14C]caffeine and its eight major metabolites in rat urine, In Journal of Chromatography B: Biomedical Sciences and Applications, Volume 726, Issues 1–2, 1999, Pages 195-201.
2. Ute Jorritsma, Eberhard Schrader, G?tz Klaunick, Jaime Kapitulnik, Karen I. Hirsch-Ernst, Georg F. Kahl, Heidi Foth, Monitoring of cytochrome P-450 1A activity by determination of the urinary pattern of caffeine metabolites in Wistar and hyperbilirubinemic Gunn rats, In Toxicology, Volume 144, Issues 1–3, 2000, Pages 229-236.