TABLE 3

Effects of endocyclic modifications in U-II on the rat thoracic aorta


Peptide

Structure

Rat Thoracic Aorta Bioassay
EC50 ± SEMa
Emax ± S.E.M.b
n c
nM %
1 ETPDCFWKYCV (hU-II) 3.3 ± 0.3 98 ± 3 12
13 ETPDCAWKYCV 1,900 ± 300 67 ± 12 4
14 ETPDCFAKYCV >10,000 N.D. 4
15 ETPDCFWAYCV >10,000 N.D. 4
16 ETPDCFWKACV >10,000 N.D. 4
18 ETPDC-WKYCV >1,000 N.D. 4
19 ETPDCF-KYCV >10,000 N.D. 4
20 ETPDCFW-YCV >10,000 N.D. 3
21 ETPDCFWK-CV >10,000 N.D. 4
22 ETPDCfWKYCV >1,000 N.D. 6
23 ETPDCFwKYCV 170 ± 50 37 ± 3 8
24 ETPDCFWkYCV >10,000 N.D. 4
25 ETPDCFWKyCV >10,000 N.D. 4
28 ETPDCFHKYCV 2,600 ± 420 52 ± 13 6
32 ETPDCFWRYCV 69 ± 15 64 ± 14 8
33 ETPDCFWOrnYCV >10,000 N.D. 4
35 ETPDCFWKFCV 35 ± 2 64 ± 14 8
36 ETPDCYWKYCV 40 ± 4 83 ± 5 9
41 ETPDCFPKYCV >10,000 69 ± 3 4
29 ETPDCAFWKYCV 2,660 ± 1,300 34 ± 4 7
40
ETPDCFKYWCV
>10,000
N.D.
5
  • N.D., not determined.

  • a Concentration producing 50% of the maximum effect.

  • b Percentage of efficacy as compared to the value obtained with 60 mM KCl.

  • c Number of animals.