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

Table 25–9
Vasopressin Receptor Antagonists
I. PEPTIDE ANTAGONISTS
O
H 2 C
CH 2 CH 2 CH2
C X Phe Y Asn Cys Pro Arg Z
1
C
2 3 4 5 6 7 8 9
CH 2 CH2
S S
A. V 1
-selective antagonists X Y Z
V 1a
-selective antagonist Tyr—OMe Gln Gly (NH 2
)
d(CH 2
) 5
[Tyr(Me) 2 ]AVP
V 1b
-selective antagonist Tyr—OMe Gln Gly (NH 2
)
dP [Tyr(Me) 2 ]AVP a,b
B. V 2
-selective antagonists a
1. des Gly-NH 29
-d(CH 2
) 5
[D-Ile 2 , Ile 4 ]AVP D-Ile Ile —
2. d(CH 2
) 5
[D-Ile 2 , Ile 4 , Ala-NH 29
]AVP D-Ile Ile Ala (NH 2
)
II. NONPEPTIDE ANTAGONISTS
A. V 1a
-selective antagonists
OPC-21268
SR 49059 (relcovaptan)
N
O
Cl
N
H
CON
N
SO 2
H
CONH 2
O
B. V 1b
-selective antagonists
O(CH 2) 3NHCOCH 3
SSR 149415
OH
O
CH 3O OCH 3
Cl
N
S
O
N
N
O O
O O
C. V 2
-selective antagonists
SR 121463A
H
OCH 2CH 2N
O
O
VPA-985 (lixivaptan)
N
CH 3CH 2O
N
O
SO 2
OCH 3
C
N
O
CH 3
Cl
N
H
CONH
F
(Continued)