[125I][Tyr26]galanin (pig)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
9.5 – 10.7
|
pKd
|
15,20,22,71,85-86
|
|
⤷ |
pKd
9.5 – 10.7
(Kd 3x10-10 – 1.9x10-11 M)
Two populations of binding sites have been identified in transfected cells with Kds of 0.3 and 0.019nM.
[15,20,22,71,85-86]
|
[125I][Tyr26]galanin (rat/mouse)
|
|
|
|
|
|
|
|
|
|
|
Mm |
Agonist |
9.9
|
pKd
|
98
|
|
⤷ |
pKd
9.9
(Kd 1.34x10-10 M)
[98]
|
[125I][Tyr26]galanin (pig)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
9.8
|
pKd
|
11
|
|
⤷ |
pKd
9.8
(Kd 1.5x10-10 M)
[11]
|
[19Lys,26Leu]-galparan
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
9.1
|
pKd
|
46
|
|
⤷ |
pKd
9.1
(Kd 7.1x10-10 M)
[46]
|
galanin
{Sp: Pig}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
9.1
|
pKd
|
46
|
|
⤷ |
pKd
9.1
(Kd 7.4x10-10 M)
[46]
|
galanin
{Sp: Pig}
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
9.1
|
pKd
|
29
|
|
⤷ |
pKd
9.1
(Kd 8x10-10 M)
[29]
|
[125I][Tyr26]galanin (human)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
7.8 – 10.3
|
pKd
|
24
|
|
⤷ |
pKd
10.3
(Kd 4.89x10-11 M)
High affinity receptors
[24]
pKd
7.8
(Kd 1.47x10-8 M)
Low affinity receptors
[24]
|
galparan
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
8.2
|
pKd
|
46
|
|
⤷ |
pKd
8.2
(Kd 6.4x10-9 M)
[46]
|
galanin(1-13)amide
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
6.9
|
pKd
|
46
|
|
⤷ |
pKd
6.9
(Kd 1.25x10-7 M)
[46]
|
[2Ala]-galparan
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
5.8
|
pKd
|
46
|
|
⤷ |
pKd
5.8
(Kd 1.585x10-6 M)
[46]
|
galanin
{Sp: Pig}
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
9.6 – 10.6
|
pKi
|
11,24,29
|
|
⤷ |
pKi
9.6 – 10.6
(Ki 2.3x10-10 – 2.5x10-11 M)
[11,24,29]
|
galanin
{Sp: Mouse, Rat}
|
|
|
|
|
|
|
|
|
|
|
Mm |
Full agonist |
9.3 – 10.3
|
pKi
|
70,98
|
|
⤷ |
pKi
9.3 – 10.3
(Ki 4.6x10-10 – 4.7x10-11 M)
[70,98]
|
galanin
{Sp: Human}
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
9.1 – 10.5
|
pKi
|
11,24,29,82
|
|
⤷ |
pKi
9.1 – 10.5
(Ki 8x10-10 – 3.1x10-11 M)
[11,24,29,82]
|
M617
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
9.6
|
pKi
|
55
|
|
⤷ |
pKi
9.6
(Ki 2.3x10-10 M)
[55]
|
M242
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
9.6
|
pKi
|
82
|
|
⤷ |
pKi
9.6
(Ki 2.5x10-10 M)
[82]
|
galanin
{Sp: Mouse, Rat}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
9.0 – 10.1
|
pKi
|
15,86,94,96-97
|
|
⤷ |
pKi
9.0 – 10.1
(Ki 1x10-9 – 8x10-11 M)
[15,86,94,96-97]
|
galanin
{Sp: Pig}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
9.1 – 10.0
|
pKi
|
15,71,85-86
|
|
⤷ |
pKi
9.1 – 10.0
(Ki 8.2x10-10 – 1x10-10 M)
[15,71,85-86]
|
galanin
{Sp: Human}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
9.2 – 9.9
|
pKi
|
15,86
|
|
⤷ |
pKi
9.2 – 9.9
(Ki 6x10-10 – 1.4x10-10 M)
[15,86]
|
galanin
{Sp: Mouse, Rat}
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
8.8 – 10.1
|
pKi
|
11,29,53,55,78,81,88
|
|
⤷ |
pKi
8.8 – 10.1
(Ki 1.75x10-9 – 8x10-11 M)
[11,29,53,55,78,81,88]
|
Gal-(K)4
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
9.4
|
pKi
|
106
|
|
⤷ |
pKi
9.4
(Ki 4x10-10 M)
[106]
|
Gal-B2-MPEG4
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
9.3
|
pKi
|
106
|
|
⤷ |
pKi
9.3
(Ki 5x10-10 M)
[106]
|
Gal-B2-C8
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
9.1
|
pKi
|
106
|
|
⤷ |
pKi
9.1
(Ki 7x10-10 M)
[106]
|
Gal-B2-dPEG24
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
8.9
|
pKi
|
105
|
|
⤷ |
pKi
8.9
(Ki 1.3x10-9 M)
[105]
|
Gal-B2-C10
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
8.9
|
pKi
|
106
|
|
⤷ |
pKi
8.9
(Ki 1.3x10-9 M)
[106]
|
Gal-B2-C12
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
8.9
|
pKi
|
106
|
|
⤷ |
pKi
8.9
(Ki 1.4x10-9 M)
[106]
|
galanin(1-16) (rat/mouse/pig)
|
|
|
|
|
|
|
|
|
|
|
Mm |
Agonist |
8.7 – 9.0
|
pKi
|
70,98
|
|
⤷ |
pKi
8.7 – 9.0
(Ki 2.2x10-9 – 1.02x10-9 M)
[70,98]
|
galanin(1-16) (rat/mouse/pig)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
8.3 – 9.3
|
pKi
|
11,14,24,29
|
|
⤷ |
pKi
8.3 – 9.3
(Ki 5x10-9 – 5x10-10 M)
[11,14,24,29]
|
Gal-B2-C14
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
8.6
|
pKi
|
106
|
|
⤷ |
pKi
8.6
(Ki 2.6x10-9 M)
[106]
|
galanin(1-16) (rat/mouse/pig)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
8.1 – 9.0
|
pKi
|
15,71,85-86,94,96-97
|
|
⤷ |
pKi
8.1 – 9.0
(Ki 9x10-9 – 9.5x10-10 M)
[15,71,85-86,94,96-97]
|
Gal-B2
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
8.5
|
pKi
|
14
|
|
⤷ |
pKi
8.5
(Ki 3.5x10-9 M)
[14]
|
Gal-B2-C18
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
8.4
|
pKi
|
106
|
|
⤷ |
pKi
8.4
(Ki 4x10-9 M)
[106]
|
galanin(1-15)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
7.9 – 8.5
|
pKi
|
71,85
|
|
⤷ |
pKi
7.9 – 8.5
(Ki 1.15x10-8 – 3x10-9 M)
[71,85]
|
galanin(7-29) (pig)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
8.2
|
pKi
|
11
|
|
⤷ |
pKi
8.2
(Ki 6.76x10-9 M)
[11]
|
galanin(2-29) (pig)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
7.1 – 8.1
|
pKi
|
15,71
|
|
⤷ |
pKi
7.1 – 8.1
(Ki 8.25x10-8 – 7.14x10-9 M)
[15,71]
|
galanin(7-29) (pig)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
7.6
|
pKi
|
86
|
|
⤷ |
pKi
7.6
(Ki 2.455x10-8 M)
[86]
|
J20 (galanin analogue)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
7.6
|
pKi
|
79
|
|
⤷ |
pKi
7.6
(Ki 2.5x10-8 M)
[79]
|
galanin(2-29) (pig)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.6
|
pKi
|
11
|
|
⤷ |
pKi
7.6
(Ki 2.63x10-8 M)
[11]
|
galanin(2-29) (rat/mouse)
|
|
|
|
|
|
|
|
|
|
|
Mm |
Full agonist |
7.1 – 8.0
|
pKi
|
70,98
|
|
⤷ |
pKi
7.1 – 8.0
(Ki 8.46x10-8 – 1.08x10-8 M)
[70,98]
|
galanin(2-30) (human)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
7.3
|
pKi
|
17
|
|
⤷ |
pKi
7.3
(Ki 5.2x10-8 M)
[17]
|
M1151
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
7.0
|
pKi
|
81
|
|
⤷ |
pKi
7.0
(Ki 9.86x10-8 M)
[81]
|
J18 (galanin analogue)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
6.9
|
pKi
|
79
|
|
⤷ |
pKi
6.9
(Ki 1.38x10-7 M)
[79]
|
galanin(2-29) (rat/mouse)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
6.0 – 7.1
|
pKi
|
94,96-97
|
|
⤷ |
pKi
6.0 – 7.1
(Ki 1.1x10-6 – 8.5x10-8 M)
[94,96-97]
|
[N-Me,des-Sar]Gal-B2
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
6.4
|
pKi
|
77
|
|
⤷ |
pKi
6.4
(Ki 3.645x10-7 M)
[77]
|
Gal-B5
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
6.4
|
pKi
|
14
|
|
⤷ |
pKi
6.4
(Ki 3.87x10-7 M)
[14]
|
M1145
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
6.2
|
pKi
|
78
|
|
⤷ |
pKi
6.2
(Ki 5.87x10-7 M)
[78]
|
galanin(D-Trp2) (pig)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
6.2
|
pKi
|
11
|
|
⤷ |
pKi
6.2
(Ki 6.31x10-7 M)
[11]
|
galanin(D-Trp2) (pig)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
6.0 – 6.4
|
pKi
|
85-86
|
|
⤷ |
pKi
6.0 – 6.4
(Ki 1x10-6 – 4.074x10-7 M)
[85-86]
|
galanin(3-29) (pig)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
<6.0
|
pKi
|
15,71,85-86
|
|
⤷ |
pKi
<6.0
(Ki >1x10-6 M)
[15,71,85-86]
|
galanin(3-29) (rat/mouse)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
<6.0
|
pKi
|
94,97
|
|
⤷ |
pKi
<6.0
(Ki >1x10-6 M)
[94,97]
|
galanin(10-29) (pig)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
<6.0
|
pKi
|
71
|
|
⤷ |
pKi
<6.0
(Ki >1x10-6 M)
[71]
|
galanin(3-29) (rat/mouse)
|
|
|
|
|
|
|
|
|
|
|
Mm |
Agonist |
<5.8
|
pKi
|
70
|
|
⤷ |
pKi
<5.8
(Ki >1.65x10-6 M)
[70]
|
galanin(10-29) (rat/mouse)
|
|
|
|
|
|
|
|
|
|
|
Mm |
Agonist |
<5.8
|
pKi
|
70
|
|
⤷ |
pKi
<5.8
(Ki >1.67x10-6 M)
[70]
|
M1153
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
5.7
|
pKi
|
81
|
|
⤷ |
pKi
5.7
(Ki 1.89x10-6 M)
[81]
|
M1152
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
5.6
|
pKi
|
81
|
|
⤷ |
pKi
5.6
(Ki 2.37x10-6 M)
[81]
|
galanin(3-29) (pig)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
<5.0 – 6.0
|
pKi
|
11,29
|
|
⤷ |
pKi
<5.0 – 6.0
(Ki >1x10-5 – 1x10-6 M)
[11,29]
|
galanin(2-11)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
<5.3
|
pKi
|
53
|
|
⤷ |
pKi
<5.3
(Ki >5x10-6 M)
[53]
|
galnon
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
4.9
|
pKi
|
5,87
|
|
⤷ |
pKi
4.9
(Ki 1.17x10-5 M)
[5,87]
|
M1160
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
4.8
|
pKi
|
80
|
|
⤷ |
pKi
4.8
(Ki 1.55x10-5 M)
[80]
|
galmic
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
4.5
|
pKi
|
5,87
|
|
⤷ |
pKi
4.5
(Ki 3.42x10-5 M)
[5,87]
|
galanin
{Sp: Mouse, Rat}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
9.8
|
pEC50
|
68
|
|
⤷ |
pEC50
9.8
(EC50 1.6x10-10 M)
[68]
|
galanin-like peptide
{Sp: Pig}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
7.5
|
pEC50
|
68
|
|
⤷ |
pEC50
7.5
(EC50 3x10-8 M)
[68]
|
galanin
{Sp: Human}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
10.1 – 10.2
|
pIC50
|
33,91
|
|
⤷ |
pIC50
10.1 – 10.2
(IC50 7x10-11 – 6x10-11 M)
[33,91]
|
galanin
{Sp: Pig}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
10.1 – 10.2
|
pIC50
|
33,91
|
|
⤷ |
pIC50
10.1 – 10.2
(IC50 7x10-11 – 6x10-11 M)
[33,91]
|
galanin
{Sp: Mouse, Rat}
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
9.9
|
pIC50
|
22
|
|
⤷ |
pIC50
9.9
(IC50 1.3x10-10 M)
[22]
|
galanin
{Sp: Pig}
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
9.8 – 9.9
|
pIC50
|
22,91
|
|
⤷ |
pIC50
9.8 – 9.9
(IC50 1.6x10-10 – 1.4x10-10 M)
[22,91]
|
galanin(1-19) (human)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
9.8
|
pIC50
|
91
|
|
⤷ |
pIC50
9.8
(IC50 1.5x10-10 M)
[91]
|
galanin
{Sp: Human}
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
9.6 – 9.9
|
pIC50
|
22,49,91
|
|
⤷ |
pIC50
9.6 – 9.9
(IC50 2.7x10-10 – 1.3x10-10 M)
[22,49,91]
|
galanin(1-16) (rat/mouse/pig)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
9.6
|
pIC50
|
33,91
|
|
⤷ |
pIC50
9.6
(IC50 2.7x10-10 M)
[33,91]
|
galanin(1-19) (human)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
9.5
|
pIC50
|
91
|
|
⤷ |
pIC50
9.5
(IC50 3.4x10-10 M)
[91]
|
galanin
{Sp: Mouse, Rat}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
8.9 – 10.0
|
pIC50
|
13,68
|
|
⤷ |
pIC50
8.9 – 10.0
(IC50 1.4x10-9 – 9.7x10-11 M)
[13,68]
|
[Sar1, D-Ala12]galanin(1-16)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
9.4
|
pIC50
|
47
|
|
⤷ |
pIC50
9.4
(IC50 4x10-10 M)
[47]
|
galanin(1-16) (rat/mouse/pig)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
9.0 – 9.2
|
pIC50
|
22,91
|
|
⤷ |
pIC50
9.0 – 9.2
(IC50 1.01x10-9 – 6x10-10 M)
[22,91]
|
galanin(1-11)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
9.0
|
pIC50
|
49
|
|
⤷ |
pIC50
9.0
(IC50 1.1x10-9 M)
[49]
|
galanin(1-15)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
8.8
|
pIC50
|
22
|
|
⤷ |
pIC50
8.8
(IC50 1.68x10-9 M)
[22]
|
galanin-like peptide
{Sp: Pig}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
8.4
|
pIC50
|
68
|
|
⤷ |
pIC50
8.4
(IC50 4.3x10-9 M)
[68]
|
galanin(2-29) (rat/mouse)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
8.1
|
pIC50
|
33,91
|
|
⤷ |
pIC50
8.1
(IC50 7.2x10-9 M)
[33,91]
|
galanin(2-29) (rat/mouse)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
8.0
|
pIC50
|
91
|
|
⤷ |
pIC50
8.0
(IC50 1x10-8 M)
[91]
|
galanin(2-29) (pig)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.5
|
pIC50
|
22
|
|
⤷ |
pIC50
7.5
(IC50 3.04x10-8 M)
[22]
|
GALP(3-32) (human)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
7.5
|
pIC50
|
44
|
|
⤷ |
pIC50
7.5
(IC50 3.3x10-8 M)
[44]
|
galanin-like peptide
{Sp: Rat}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
7.3
|
pIC50
|
13
|
|
⤷ |
pIC50
7.3
(IC50 4.5x10-8 M)
[13]
|
galanin-like peptide
{Sp: Human}
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
7.1
|
pIC50
|
44
|
|
⤷ |
pIC50
7.1
(IC50 7.7x10-8 M)
[44]
|
GALP(1-32) (human)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
6.9
|
pIC50
|
44
|
|
⤷ |
pIC50
6.9
(IC50 1.29x10-7 M)
[44]
|
galanin(2-11)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
6.1
|
pIC50
|
49
|
|
⤷ |
pIC50
6.1
(IC50 8.79x10-7 M)
[49]
|
galanin(3-29) (pig)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
<6.0
|
pIC50
|
22
|
|
⤷ |
pIC50
<6.0
(IC50 >1x10-6 M)
[22]
|
galanin(3-29) (rat/mouse)
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
<6.0
|
pIC50
|
91
|
|
⤷ |
pIC50
<6.0
(IC50 >1x10-6 M)
[91]
|
galanin(3-29) (rat/mouse)
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
<6.0
|
pIC50
|
33,91
|
|
⤷ |
pIC50
<6.0
(IC50 >1x10-6 M)
[33,91]
|
alarin
{Sp: Rat}
|
|
|
|
|
|
|
|
|
|
|
Rn |
Agonist |
<6.0
|
pIC50
|
13
|
|
⤷ |
pIC50
<6.0
(IC50 >1x10-6 M)
[13]
|