Enkephalin (2-D-Alanine-5-D-Leucine), [Tyrosyl-3,5-3H(N)]-, 250µCi (9.25MBq)

DADLE acts as an agonist at delta opioid receptors (DOR), but has also been shown to bind mu opioid receptors (MOR). These receptors are a group of GPCRs that are potential drug targets for pain and drug addiction.

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 NET648:

1. Vo?ahlíková, M., Jurkiewicz, P., Roubalová, L. et al. (2014), High- and low-affinity sites for sodium in δ-OR-Gi1α (Cys351-Ile351) fusion protein stably expressed in HEK293 cells; functional significance and correlation with biophysical state of plasma membrane. Naunyn-Schmiedeberg's Arch Pharmacol, 387: 487.
2. Bourova, L., Kostrnova, A., Hejnova, L., Moravcova, Z., Moon, H.-E., Novotny, J., Milligan, G. and Svoboda, P. (2003), δ-Opioid receptors exhibit high efficiency when activating trimeric G proteins in membrane domains. Journal of Neurochemistry, 85: 34–49.