Butyl Bicyclophosphorothionate, Tertiary-[³⁵S]-, 100µCi (3.7MBq), Ethanol under nitrogen

t-Butylbicyclophosphorothionate (TBPS) is a byciclophosphate derivative that binds with high affinity and specificity to GABA_A receptors. GABA_A receptors are the main fast inhibitor neurotransmitter receptors in the human brain, and are potential drug targets for anxiety, insomnia, and anesthesia.

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 NEG049:

1. Casida, J E, and L J Lawrence. Structure-Activity Correlations for Interactions of Bicyclophosphorus Esters and Some Polychlorocycloalkane and Pyrethroid Insecticides with the Brain-Specific T-Butylbicyclophosphorothionate Receptor. Environmental Health Perspectives 61 (1985): 123–132.
2. Pitkänen, A., Saano, V., Tuomisto, L. and Riekkinen, P. J. (1987), Effect of Anticonvulsant Drugs on (35S)t-Butylbicyclophosphorothionate Binding in Vitro and ex Vivo. Pharmacology & Toxicology, 61: 103–106.