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DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

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Table 32–3

Structure of Kinin Agonists and Antagonists

NAME STRUCTURE FUNCTION

Bradykinin Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg Agonist, B 2

Kallidin Lys-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg Agonist, B 2

[des-Arg 9 ]-bradykinin Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe Agonist, B 1

[des-Arg 10 ]-kallidin Lys-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe Agonist, B 1

des-Arg 10 -[Leu 9 ]-kallidin Lys-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Leu Antagonist, B 1

NPC-349 [D-Arg]-Arg-Pro-Hyp-Gly-Thi-Ser-D-Phe-Thi-Arg Antagonist, B 2

HOE-140 [D-Arg]-Arg-Pro-Hyp-Gly-Thi-Ser-Tic-Oic-Arg Antagonist, B 2

[des-Arg 10 ]-HOE-140 [D-Arg]-Arg-Pro-Hyp-Gly-Thi-Ser-Tic-Oic Antagonist, B 1

N

FR173657 O

Antagonist, B 2

Cl

Cl

O

N

H

N

O

N

NHAc

O

N

N

FR190997 Agonist, B 2

O

O

Cl

Cl

O

N

H

N

O

N

H

SSR240612 Antagonist, B 1

ABBREVIATIONS: Hyp, trans-4-hydroxy-Pro; Thi, β-(2-thienyl)-Ala; Tic, [D]-1,2,3,4-tetrahydroisoquinolin-3-yl-carbonyl; Oic, (3as,7as)-octahydroindol-2-yl-carbonyl.

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