Synthesis, biological activity and receptor binding affinity of six new antagonists of [8-L-arginine]vasopressin

1989 ◽  
Vol 54 (12) ◽  
pp. 3374-3380 ◽  
Author(s):  
Bernard Lammek ◽  
Izabela Derdowska ◽  
Gotfryd Kupryszewski ◽  
Jiřina Slaninová ◽  
Tomislav Barth ◽  
...  
Keyword(s):  
Biological Activity ◽  
Binding Affinity ◽  
Receptor Binding ◽  
Arginine Vasopressin ◽  
Strong Decrease ◽  
Inhibitory Potency ◽  
Receptor Binding Affinity ◽  
Biological Potency

Six analogues of d(CH2)5AVP, a vasopressin inhibitor, modified in positions 1, 2, 4, and 9 were synthesized and the effect of the modifications on the inhibitory potency was followed. Buly and lipophilic substitutions in position 1 in combination with Abu substitution in position 4 led to a slight decrease of antivasopressor potency and a strong decrease of the antiuterotonic potency. Alkylation of any type of carboxamide group at positions 4 and 9 strongly reduced the biological potency in all the tests.

scholarly journals Endothelin receptor binding affinity and biological activity of a novel endothelin analog, KET-023.

1991 ◽  
Vol 55 ◽  
pp. 269
Author(s):  
Hirpkazu Akiyama ◽  
Ypghimasa Inagaki ◽  
Tomoko Kashiwabara ◽  
Hideo Ohta ◽  
Akihito Morita ◽  
...  
Keyword(s):  
Biological Activity ◽  
Binding Affinity ◽  
Receptor Binding ◽  
Endothelin Receptor ◽  
Receptor Binding Affinity

scholarly journals Receptor binding affinity and biological activity of varied length of peptides elongated from C-terminal of endothelin

1990 ◽  
Vol 52 ◽  
pp. 203
Author(s):  
Hirokazu Akiyama ◽  
Yoshimasa Inagaki ◽  
Hideo Ohta ◽  
Tomoko Kashiwabara ◽  
Akihiro Iwamatsu ◽  
...  
Keyword(s):  
Biological Activity ◽  
Binding Affinity ◽  
Receptor Binding ◽  
Receptor Binding Affinity

Divergence of the in vitro biological activity and receptor binding affinity of a synthetic insulin analog. [21-Asparaginamide-A]insulin

Biochemistry ◽  
1980 ◽  
Vol 19 (20) ◽  
pp. 4547-4556 ◽  
Author(s):  
G. Thompson Burke ◽  
Jacob D. Chanley ◽  
Yoshio Okada ◽  
Alexandros Cosmatos ◽  
Nicolaos Ferderigos ◽  
...  
Keyword(s):  
Biological Activity ◽  
Binding Affinity ◽  
Receptor Binding ◽  
Insulin Analog ◽  
Receptor Binding Affinity

scholarly journals Endothelin receptor binding affinity and biological activity of a novel endothelin analog, KET-011

1992 ◽  
Vol 58 ◽  
pp. 336
Author(s):  
Hirokazu Akiyama ◽  
Yoshimasa Inagaki ◽  
Tomoko Kashiwabara ◽  
Hideo Ohta ◽  
Hideaki Fukushima ◽  
...  
Keyword(s):  
Biological Activity ◽  
Binding Affinity ◽  
Receptor Binding ◽  
Endothelin Receptor ◽  
Receptor Binding Affinity

Insulin analog possessing higher in vitro biological activity than receptor binding affinity. [21-Proline-B]insulin

Biochemistry ◽  
1983 ◽  
Vol 22 (19) ◽  
pp. 4561-4567 ◽  
Author(s):  
Gerald P. Schwartz ◽  
G. Thompson Burke ◽  
Jacob D. Chanley ◽  
Panayotis G. Katsoyannis
Keyword(s):  
Biological Activity ◽  
Binding Affinity ◽  
Receptor Binding ◽  
Insulin Analog ◽  
Receptor Binding Affinity

Receptor binding affinity and biological activity of C-terminal elongated forms of endothelin-1

1991 ◽  
Vol 18 (4) ◽  
pp. 535-539 ◽  
Author(s):  
Koji Nishikori ◽  
Hirokazu Akiyama ◽  
Yoshimasa Inagaki ◽  
Hideo Ohta ◽  
Tomoko Kashiwabara ◽  
...  
Keyword(s):  
Biological Activity ◽  
Binding Affinity ◽  
Receptor Binding ◽  
Receptor Binding Affinity ◽  
Endothelin 1
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