Tyramine is a biogenic monoamine commonly found in invertebrates and is the synthetic precursor to octopamine.  Tyramine and octopamine exert various physiological/biochemical actions by interacting with G-Protein-Coupled Receptors (GPCRs).  Octopamine receptors are well studied and have a defined pharmacological profile; tyramine receptors are not as well studied.  Octopamine receptors are believed to be the target of formamidine insecticides.  Previously, a putative octopamine receptor was isolated from amitraz-susceptible and amitraz-resistant southern cattle tick (Rhipicephalus microplus), but its ligand was never confirmed.  The amitraz-resistant receptor displayed two nucleotide substitutions.  Expression of these putative receptors in Chinese hamster ovary (CHO) cells resulted in a 41-fold higher functional response to tyramine versus octopamine.  Furthermore, the pharmacological profile was similar to known tyraminergic compounds.  Functional responses indicate that the putative octopamine receptor is actually a tyramine receptor.

Deorphanization and pharmacological profile of a tyramine receptor from the southern cattle tick (<i>Rhipicephalus microplus</i>)

246th National Meeting (2013)

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Deorphanization and pharmacological profile of a tyramine receptor from the southern cattle tick (Rhipicephalus microplus)