Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands

M P Allen; J F Blake; D K Bryce; M E Haggan; S Liras; S McLean; B E Segelstein

doi:10.1016/s0960-894x(00)00034-2

Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands

Bioorg Med Chem Lett. 2000 Mar 20;10(6):523-6. doi: 10.1016/s0960-894x(00)00034-2.

Authors

M P Allen¹, J F Blake, D K Bryce, M E Haggan, S Liras, S McLean, B E Segelstein

Affiliation

¹ CNS Discovery, Central Research Division, Pfizer Inc, Groton, CT 06340, USA.

PMID: 10741545
DOI: 10.1016/s0960-894x(00)00034-2

Abstract

3-Amino-3-phenylpropionamide derivatives were produced as small molecule mimics of the cyclic octapeptide octreotide from readily available imine 1. The compounds exhibit high affinity for the mu opioid receptor.

MeSH terms

Animals
Benzylamines / chemical synthesis*
Benzylamines / pharmacology
Brain Chemistry
CHO Cells
Cricetinae
Crystallography, X-Ray
Drug Design
Humans
Ligands
Octreotide / analogs & derivatives
Octreotide / pharmacology
Rats
Receptors, Opioid, mu / drug effects*

Substances

Benzylamines
Ligands
Receptors, Opioid, mu
3-Tyr-octreotide
Octreotide