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  • Title: Gastrointestinal neurotensin receptors: contribution of the aromatic hydroxyl group in position 11 to peptide potency.
    Author: Donoso MV, Huidobro-Toro JP, St Pierre S.
    Journal: Br J Pharmacol; 1986 Mar; 87(3):483-5. PubMed ID: 3026538.
    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 greater than [Phe11]-neurotensin greater than [D-Tyr11]-neurotensin greater than [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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