Gastrointestinal neurotensin receptors: contribution of the aromatic hydroxyl group in position 11 to peptide potency

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Abstract
Neurotensin structural analogues on tyrosine11 were tested in vitro to determine their ability to contract the fundus or relax the intestine. The rank order of potency was: neurotensin > [Phe11]-neurotensin > [D-Tyr11]-neurotensin > [D-Phe11]-neurotensin. All peptides behaved as full agonists. It is concluded that tyrosine11 is part of the neurotensin pharmacophore; the hydroxyl group increases the affinity not the intrinsic activity of the peptide at the receptor.

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