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. 1986 Mar;87(3):483-5.
doi: 10.1111/j.1476-5381.1986.tb10189.x.

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

M V Donoso, J P Huidobro-Toro, S St Pierre

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

M V Donoso et al. Br J Pharmacol. 1986 Mar.

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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