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Thyrotropin receptor (TSHR) agonists and antagonists act on the receptor for thyroid-stimulating hormone. TSHR is a class A G protein-coupled receptor with a large leucine-rich extracellular domain that binds the hormone. Its complementary DNA was cloned in 1989, and receptor activation raises cyclic adenosine monophosphate (cAMP) to drive thyroid hormone synthesis and thyroid cell growth. Stimulating autoantibodies against the receptor underlie Graves' disease, so TSHR ligands are used in thyroid autoimmunity research. Small-molecule agonists were shown in 2009 to stimulate thyroid function in human thyrocytes and mice. ML-109 and MS437 act as agonists, TSHR antagonist S37a blocks receptor activation, and ML224 is an inverse agonist that lowers basal signaling.
Org41841 is a partial agonist of both luteinizing hormone/chorionic gonadotropin receptor (LHCGR) and thyroid-stimulating hormone receptor (TSHR) with EC50s of 0.2 and 7.7 μM, respectively.
