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Steady state studies varying NADPH and inhibitor concentrations indicate that treatment with the fast inhibitors 7 and 8 or the slow inhibitor 3 , (the only slow inhibitor reaching equilibrium in 6 h), resulted in decreases in both K m and V max values consistent with uncompetitive inhibition of TGR, while treatment with 9 , a close analog of compound 8 synthesized ad hoc to facilitate structural studies (see below), changed only the V max indicating noncompetitive inhibition (Supplementary Tables 15 and 16)

This Gq/11-coupled receptor is expressed primarily in somatotropic cells of the anterior pituitary and in certain hypothalamic areas (arcuate nucleus, paraventricular nucleus)

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The dosing described was conservative by peptide therapy standards