MK-912, [³H(G)]

MK-912 functions as a α2-adrenoceptor antagonist. It is used in studies looking at regulation of cardiovascular and CNS functions. This compound replaces NET1059.

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 NET1227:

1. A Drews, J.-J Pietzsch, R Syhe, S Seifert, K Varanas, H Hall, C Halldin, W Kraus, P Karlsson, C Johnsson, H Spies, B Johannsen. Synthesis and biological evaluation of technetium (III) mixed-ligand complexes with high affinity for the cerebral 5-HT_1A receptor with the alpha1-adenergic receptor. Nuclear Medicine and Biology. May 2002. Volume 29, Issue 4, page 389-398.