Biomedical Engineering Reference
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NH
NH
O
O
H
N
H
N
N
H
NH
2
N
H
NH
2
O
N
O
S
O
O
O
O
O
O
sstr2
sstr2
N
Et
N
O
O
HN
H
NH
2
NH
N
N
Et
H
2
N
S
O
sstr3
O
sstr5
O
Figure 3.48 Somatostatin mimetic antagonists
H
N
NH
NH
N
H
2
N
O
O
O
O
HN
O
HN
Ph
H
H
H
N
N
N
NH
2
NH
2
H
O
O
OH
O
OH
H
N
NH
O
O
HN
N
NH
2
O
Figure 3.49 Somatostatin mimetics based on b-org-homo amino acids
The structural similarity of the somatostatin pharmacophore with that of
urotensin (U-II) stimulated the application of the established somatostatin
SAR to U-II. U-II is a cyclic undecapeptide with potent vasoactive properties
(Figure 3.51). The endocyclic residues were shown to be critical for biolo-
gical activity.
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