標識リガンド一覧

GPCRs：　　数字 | A | B | C | D | E | F | G | H | K | L | M | N | O | P | R | S | T | U | V

Transporters

Ligand-gated ion channels

Voltage-gated ion channels

Nuclear receptors

 

GPCRs すべて展開　|　すべて折り畳む

5-Hydroxytryptamine （Serotonin）

Subtype G-protein coupling Radioligand Pharmacological action
5-HT1A Gi/Go 5-CT, [3H]- agonist
5-CT, TFA, [3H]- agonist
8-OH-DPAT, [3H]- agonist
MPPF, [3H]- 5-HT1A antagonist
p-MPPI, [125I]- 5-HT1A antagonist
WAY-100635, [methoxy-3H] 5-HT1A antagonist
Ketanserin HCl, [3H]- antagonist
Spiperone, [benzene ring-3H]- antagonist
Spiperone, [3H]- antagonist
Yohimbine, [3H]- antagonist
GR 125,743, [3H]- antagonist
5-HT1B Gi/G0 5-CT, [3H]- agonist
5-CT, TFA, [3H]- agonist
8-OH-DPAT, [3H]- agonist
Ketanserin HCl, [3H]- antagonist
Spiperone, [benzene ring-3H]- antagonist
Spiperone, [3H]- antagonist
Rauwolscine, [3H]- antagonist
Yohimbine, [3H]- antagonist
GR 125,743, [3H]- antagonist
5-HT1D Gi/G0 5-CT, [3H]- agonist
5-CT, TFA, [3H]- agonist
8-OH-DPAT, [3H]- agonist
Ketanserin HCl, [3H]- antagonist
Spiperone, [benzene ring-3H]- antagonist
Spiperone, [3H]- antagonist
Rauwolscine, [3H]- antagonist
Yohimbine, [3H]- antagonist
5-ht1e Gi/G0 8-OH-DPAT, [3H]- agonist
Rauwolscine, [3H]- antagonist
Yohimbine, [3H]- antagonist
5-HT1F Gi/G0 8-OH-DPAT, [3H]- agonist
Yohimbine, [3H]- antagonist
5-HT2A Gq/G11 8-OH-DPAT, [3H]- agonist
Ketanserin HCl, [3H]- antagonist
Mesulergine, [3H]- antagonist
Spiperone, [benzene ring-3H]- antagonist
Spiperone, [3H]- antagonist
5-HT2B Gq/G11 8-OH-DPAT, [3H]- agonist
Ketanserin HCl, [3H]- antagonist
Mesulergine, [3H]- antagonist
Spiperone, [benzene ring-3H]-, antagonist
Spiperone, [3H]- antagonist
Rauwolscine, [3H]- antagonist
Yohimbine, [3H]- antagonist
5-HT2C Gq/G11 8-OH-DPAT, [3H]- agonist
Ketanserin HCl, [3H]- antagonist
Mesulergine, [3H]- inverse agonist
Spiperone, [benzene ring-3H]-, antagonist
Spiperone, [3H]- antagonist
5-HT3 (See Ligand-gated channel)
5-HT4 GS GR 113808, [3H]- 5-HT4 antagonist
5-ht5a Gi/G0 5-CT, [3H]- agonist
5-CT, TFA, [3H]- agonist
8-OH-DPAT, [3H]- agonist
[125I]-LSD agonist
Ketanserin HCl, [3H]- antagonist
Yohimbine, [3H]- antagonist
5-HT6 Gs Mesulergine, [3H]- antagonist
SB 258585, [125I]- 5-HT6 antagonist
5-HT7 Gs 5-CT, [3H]- agonist
5-CT, TFA, [3H]- agonist
8-OH-DPAT, [3H]- agonist
[125I]-LSD agonist
Ketanserin HCl, [3H]- antagonist
Mesulergine, [3H]- antagonist
SB 269970, [3H]- antagonist
Yohimbine, [3H]- antagonist
    5-Hydroxytryptamine creatinine sulfate, [1,2-3H(N)]- endogenous
5-Hydroxytryptamine trifluoroacetate, [aminoethyl-3H]- endogenous

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Acetylcholine (Muscarinic)

Subtype G-protein coupling Radioligand Pharmacological action
M1 Gq/G11 Oxotremorine-M acetate, [methyl-3H]- M1 - M5 agonist
4-DAMP, [N-methyl-3H]- M1, M3 antagonist
NMS, [N-methyl-3H]- M1 - M5 antagonist
Pirenzepine, [N-methyl-3H]- M1 antagonist
QNB, L-[benzilic-4,4'-3H]- M1 - M5 antagonist
M2 Gi/Go Oxotremorine-M acetate, [methyl-3H]- M1 - M5 agonist
AF-DX 384, [2,3-dipropylamino-3H]- M2 antagonist
4-DAMP, [N-methyl-3H]- M1, M3 antagonist
NMS, [N-methyl-3H]- M1 - M5 antagonist
QNB, L-[benzilic-4,4'-3H]- M1 - M5 antagonist
M3 Gq/G11 Oxotremorine-M acetate, [methyl-3H]- M1 - M5 agonist
4-DAMP, [N-methyl-3H]- M1, M3 antagonist
NMS, [N-methyl-3H]- M1 - M5 antagonist
QNB, L-[benzilic-4,4'-3H]- M1 - M5 antagonist
M4 Gi/Go Oxotremorine-M acetate, [methyl-3H]- M1 - M5 agonist
NMS, [N-methyl-3H]- M1 - M5 antagonist
QNB, L-[benzilic-4,4'-3H]- M1 - M5 antagonist
M5 Gq/G11 Oxotremorine-M acetate, [methyl-3H]- M1 - M5 agonist
NMS, [N-methyl-3H]- M1 - M5 antagonist
QNB, L-[benzilic-4,4'-3H]- M1 - M5 antagonist
Acetylcholine iodide, [acetyl-3H]- endogenous

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Acetylcholine (Nicotinic) (See Ligand-gated ion channels)

Adenosine

Subtype G-protein coupling Radioligand Pharmacological action
A1 Gi/Go NECA, 5'-N-[adenine-2,8-3H]- agonist
DPCPX, [dipropyl-2,3-3H(N)]- antagonist
A2A Gs AB-MECA, [125I]- A2, A3 agonist
CGS 21680, [carboxyethyl-3H(N)]- A2 agonist
NECA, 5'-N-[adenine-2,8-3H]- agonist
DPCPX, [dipropyl-2,3-3H(N)]- antagonist
A2B Gs AB-MECA, [125I]- A2, A3 agonist
CGS 21680, [carboxyethyl-3H(N)]- A2 agonist
NECA, 5'-N-[adenine-2,8-3H]- agonist
DPCPX, [dipropyl-2,3-3H(N)]- antagonist
A3 Gi/Go AB-MECA, [125I]- A2, A3 agonist
NECA, 5'-N-[adenine-2,8-3H]- agonist
DPCPX, [dipropyl-2,3-3H(N)]- antagonist

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Adrenoceptors

Subtype G-protein coupling Radioligand Pharmacological action
α1A
α1D		 Gq/G11 HEAT, [125I]- agonist
Prazosin, [7-methoxy-3H]- inverse agonist
Ketanserin HCl, [3H]- antagonist
Spiperone, [benzene ring-3H]- antagonist
Spiperone, [3H]- antagonist
α1B Gq/G11 HEAT, [125I]- agonist
Prazosin, [7-methoxy-3H]- inverse agonist
Spiperone, [benzene ring-3H]- inverse agonist
Spiperone, [3H]- inverse agonist
Ketanserin HCl, [3H]- antagonist
α2A
α2B
α2C		 Gi/Go Clonidine HCl, [benzene ring-3H]- partial agonist
p-Iodoclonidine, [125I]- agonist
UK-14,304, [imidazolyl-4,5-3H]- agonist
Rauwolscine, [methyl-3H]- antagonist
Yohimbine, [methyl-3H]- antagonist
MK-912, [methyl-3H]- antagonist
RX781094, [3H]- antagonist
RX821002, [3H] antagonist
β1
β2
β3		 Gs (-)-CGP 12177, [5,7-3H]- antagonist
(-)-Cyanopindolol, [125I]- antagonist
(+/-)-Cyanopindolol, [125I]- antagonist
Dihydroalprenolol HCl, levo [ring, propyl-3H]- antagonist
(-)-Pindolol, [125I]- antagonist
Propranolol, L-[4-3H]- antagonist
Epinephrine, levo-[N-methyl-3H]- endogenous
Norepinephrine, levo-[ring-2,5,6-3H]- endogenous

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Anaphylatoxin

Subtype G-protein coupling Radioligand Pharmacological action
C3a Gi/Go Complement C3a , [125I]Bolton-Hunter labeled C3a endogenous
C5a Gi/Go Complement C5a , [125I]Bolton-Hunter labeled C5a endogenous

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Angiotensin

Subtype G-protein coupling Radioligand Pharmacological action
AT1 Gi/G0
Gq/G11		 Angiotensin I, [125I]Tyr4- endogenous
Angiotensin II, [125I]Tyr4- endogenous
Angiotensin IV, [125I]Tyr2 Non AT1, non AT2 agonist
Angiotensin II (Sar1, Ile8), [125I]Tyr4- AT antagonist
AT2 Gi/Go Angiotensin II, [125I]Tyr4- endogenous
Angiotensin IV, [125I]Tyr2 Non AT1, non AT2 agonist
CGP42112A, [125I]- AT2 partial agonist
Angiotensin II (Sar1, Ile8), [125I]Tyr4- AT antagonist

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Apelin

Subtype G-protein coupling Radioligand Pharmacological action
APJ Gi/Go Apelin 13 (Glp65, Nle75, [125I]Tyr77) APJ agonist

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Bombesin

Subtype G-protein coupling Radioligand Pharmacological action
BB1 Gq/G11 Bombesin ([125I]Tyr4) agonist
GRP (Porcine), [125I]Tyr15- agonist
BB2 Gq/G11 Bombesin ([125I]Tyr4) agonist
GRP (Porcine), [125I]Tyr15- agonist
BB3 Gq/G11 Bombesin (6-14) (D-[125I]Tyr6, βAla11, Phe13, Nle14) BB3 agonist
Bombesin ([125I]Tyr4) agonist

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Bradykinin

Subtype G-protein coupling Radioligand Pharmacological action
B1 Gi/G0
Gq/G11		 Kallidin (Des-Arg10), [3,4-prolyl-3,4-3H(N)]- B1 agonist
Kallidin (Des-Arg10, Leu9), [3,4-prolyl-3,4-3H(N)]- B1 antagonist
Bradykinin, [2,3-prolyl-3,4-3H]- endogenous

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Calcitonin

Subtype G-protein coupling Radioligand Pharmacological action
CT Gs Calcitonin (human), [125I]Tyr12- agonist
Calcitonin (salmon), [125I]Tyr22- agonist
α-CGRP (human) , [125I]His10- agonist
AMY1 Gs Amylin (rat), [125I]Bolton-Hunter labeled antagonist
Calcitonin (human), [125I] Tyr12- agonist
Calcitonin (salmon), [125I]Tyr22- agonist
α-CGRP (human) , [125I]His10- agonist
AMY2 Gs Amylin (rat), [125I]Bolton-Hunter labeled antagonist
Calcitonin (human), [125I] Tyr12- agonist
α-CGRP (human) , [125I]His10- agonist
CGRP Gs α-CGRP (human) , [125I]His10- agonist
Adrenomedullin (rat), [125I]- agonist
α-CGRP (rat) , [125I]His10- agonist
AM1
AM2		 Gs α-CGRP (human) , [125I]His10- agonist
Adrenomedullin (13-52) (human), [125I] Tyr- agonist
Adrenomedullin (rat), [125I]- agonist
α-CGRP (rat) , [125I]His10- agonist

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Cannabinoid

Subtype G-protein coupling Radioligand Pharmacological action
CB1 Gi/Go CP 55940, [side chain-2,3,4-3H(N)]- agonist
WIN 55,212-2, [5,7-naphtyl-3H]- agonist
SR141716A, [3H] CB1 antagonist
CB2 Gi/Go CP 55940, [side chain-2,3,4-3H(N)]- agonist
WIN 55,212-2, [5,7-naphtyl-3H]- agonist
Anadamide, [3H]- endogenous

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Chemokine

Subtype G-protein coupling Radioligand Pharmacological action
CCR1 Gi/Go MCP-1 (CCL2), [125I]Bolton-Hunter labeled CCR1, CCR2 agonist
MIP-1α (CCL3), [125I]- CCR1, CCR5 agonist
MIP-1β (CCL4) (Leu3,Gly47), [125I]- CCR1, CCR5 agonist
RANTES (CCL5), [125I]- CCR1, CCR3, CCR5, CXCR3 agonist
CCL15, [125I]- CCR1, CCR3 agonist
CCR2 Gi/Go MCP-1 (CCL2), [125I]Bolton-Hunter labeled CCR1, CCR2, CCR3, CCR5 agonist
JE, [125I]Bolton-Hunter labeled (murine, recombinant MCP-1) CCR2 agonist
Eotaxin (CCL11), [125I]- CCR2, CCR5, CXCR3 agonist
CCR3 Gi/Go MCP-1 (CCL2), [125I]Bolton-Hunter labeled CCR1, CCR2, CCR3, CCR5 agonist
RANTES (CCL5), [125I]- CCR1, CCR3, CCR5, CXCR3 agonist
Eotaxin (CCL11), [125I]- CCR3 antagonist
CCL15, [125I]- CCR1, CCR3 agonist
CCR4 Gi/Go TARC (CCL17), [125I]- CCR4 agonist
CCR5 Gi/Go MCP-1 (CCL2), [125I]Bolton-Hunter labeled CCR1, CCR2, CCR3, CCR5 agonist
MIP-1α (CCL3), [125I]- CCR1, CCR5 agonist
MIP-1β (CCL4) (Leu3,Gly47), [125I]- CCR1, CCR5 agonist
RANTES (CCL5), [125I]- CCR1, CCR3, CCR5, CXCR3 agonist
CCR6 Gi/Go MIP-3α (CCL20), [125I]- CCR6, CXCR3 agonist
CCR7 Gi/Go MIP-3β (CCL19), [125I]- CCR7, CXCR3 agonist
6-Ckine (CCL21), [125I]Bolton-Hunter labeled CCR7 agonist
CCR8 Gi/Go I309 (CCL1), [125I]Bolton-Hunter labeled CCR8 agonist
CCR10 Gi/Go CTACK (CCL27), [125I]- CCR10  endogenous
CXCR1 Gi/Go GROa (CXCL1), [125I]- CXCR1, CXCR2 agonist
IL-8 (CXCL8), [125I]- (lyophilized) CXCR1, CXCR2 agonist
IL-8 (CXCL8), [125I]- (liquid) CXCR1, CXCR2 agonist
CXCR2 Gi/Go GROa (CXCL1), [125I]- CXCR1, CXCR2 agonist
IL-8 (CXCL8), [125I]- (lyophilized) CXCR1, CXCR2 agonist
IL-8 (CXCL8), [125I]- (liquid) CXCR1, CXCR2 agonist
CXCR3 Gi/Go RANTES (CCL5), [125I]- CCR1, CCR3, CCR5, CXCR3 agonist
Eotaxin (CCL11), [125I]- CCR2, CCR5, CXCR3 agonist
MIP-3β (CCL19), [125I]- CCR7, CXCR3 agonist
MIP-3α (CCL20), [125I]- CCR6, CXCR3 agonist
IP-10 (CXCL10), [125I]- CXCR3 agonist
I-TAC (CXCL11), [125I]- CXCR3 endogenous
SDF1α (CXCL12), [125I]- CXCR3, CXCR4 agonist
CXCR4 Gi/Go SDF1α (CXCL12), [125I]- CXCR3, CXCR4 agonist
CXCR5 Gi/Go CXCL13, [125I]- CXCR5 endogenous
CXCR6 Gi/Go CXCL16, [125I]- CXCR6 agonist
CX3CR1 Gi/Go Fractalkine (CX3CR1), [125I]- CX3CR1 agonist

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Cholecystokinin

Subtype G-protein coupling Radioligand Pharmacological action
CCK1
CCK2		 Gq/G11 CCK-8 (sulphated), [3H]propionylated endogenous
CCK-8(sulphated), [125I]Bolton-Hunter labeled agonist
Gastrin I, [125I] Tyr12- endogenous

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Corticotropin-releasing factor

Subtype G-protein coupling Radioligand Pharmacological action
CRF1 Gs CRF (human/ rat), ([125I]Tyr0) agonist
CRF (ovine), ([125I]Tyr0) (ovine) agonist
Sauvagine ([125I]Tyr0) agonist
CRF2 Gs CRF (human/ rat), ([125I]Tyr0) agonist
CRF (ovine), ([125I]Tyr0) (ovine) agonist
Sauvagine ([125I]Tyr0) agonist
Antisauvagine-30, [125I]His2- CRF2 antagonist

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Dopamine

Subtype G-protein coupling Radioligand Pharmacological action
D1 Gs SCH 23390, [N-methyl-3H]- D1, D5 antagonist
D2
D3		 Gi/Go R(+)7-OH DPAT, [3H]- D2, D3 agonist
R(+) trans-7-OH-PIPAT, [125I]- D2, D3 agonist
Quinpirole, [N-propyl-3H]- D2, D3 agonist
Domperidone, [benzene ring-3H]- D2, D3 antagonist
Iodosulpride, [125I]- D2, D3 antagonist
Methylspiperone, [N-methyl-3H]- D2, D3 antagonist
Raclopride, [methoxy-3H]- D2, D3 antagonist
YM-09151-2, [N-methyl-3H]- D2, D3 antagonist
(-)-Sulpiride, [methoxy-3H]- D2, D3, D4 antagonist
D4 Gi/Go (-)-Sulpiride, [methoxy-3H]- D2, D3, D4 antagonist
D5 Gs SCH 23390, [N-methyl-3H]- D1, D5 antagonist
    3,4-Dihydroxyphenylethylamine, [2,5,6,7,8-3H] endogenous
3,4-Dihydroxyphenylethylamine, [ring-2,5,6-3H]- endogenous
3,4-Dihydroxyphenylethylamine, [7-3H]- endogenous

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Endothelin

Subtype G-protein coupling Radioligand Pharmacological action
ETA Gq/G11 Endothelin-1, [125I]Tyr13- agonist
BQ123, [leucyl-3H]- ETA antagonist
ETB Gq/G11 Endothelin-1, [125I]Tyr13- agonist

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Formylpeptide

Subtype G-protein coupling Radioligand Pharmacological action
FPR3 Gi/Go WKYMVm, [125I]Bolton-Hunter labeled agonist

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GABA

Subtype G-protein coupling Radioligand Pharmacological action
GABAA (See Ligand-gated ion channel)
GABAB1 Gi/Go (-)-Baclofen, [butyl-4-3H(N)]- GABAB agonist
GABA, [2,3-3H(N)]- endogenous

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Galanin

Subtype G-protein coupling Radioligand Pharmacological action
GAL2
GAL3		   Galanin (2-11), [125I]- GAL2, GAL3 agonist
Galanin (porcine), [125I]- endogenous
Galanin (human), [125I]- endogenous

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Ghrelin

Subtype G-protein coupling Radioligand Pharmacological action
ghrelin Gq/G11 Ghrelin, [125I]His9- endogenous
Ghrelin ([125I]Tyr4) agonist

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Glucagon

Subtype G-protein coupling Radioligand Pharmacological action
GIP Gs GIP (human), [125I]- endogenous
GLP-1 Gs GLP-1 (7-36) amide, [125I]- GLP-1 agonist
Exendin (9-39), [125I]- GLP-1 antagonist
GLP-2   GLP-2 (1-33) (human), [125I]Bolton-Hunter labeled endogenous
glucagon Gs Glucagon, [125I]- endogenous
secretin Gs/Gq VIP, [125I]- partial agonist

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Glutamine (see metabolic Glutamate)

Gonadotrophin-releasing hormone

Subtype G-protein coupling Radioligand Pharmacological action
GnRH Gq/G11 LH-RH (D-Trp6), [125I]Tyr5- agonist
LH-RH, [125I]Tyr5- agonist

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Histamine

Subtype G-protein coupling Radioligand Pharmacological action
H1 Gq/G11 Pyrilamine, [pyridinyl 5-3H]- inverse agonist
H2 Gq/G11 Iodoaminopotentidine, [125I]- H2 antagonist
Tiotidine, [methyl-3H]- H2 antagonist
H3 Gi/Go Methylhistamine 2HCl, N-α-[methyl-3H]- H3, H4 agonist
Iodoproxyfan, [125I]- H3 antagonist
H4 Gi/Go Methylhistamine 2HCl, N-α-[methyl-3H]- H3, H4 agonist
Pyrilamine, [pyridinyl 5-3H]- antagonist
Histamine 2HCl, [ring, methylenes-3H(N)]- endogenous

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Kisspeptin (Metastin)

Subtype G-protein coupling Radioligand Pharmacological action
Kisspeptin (GPR54) Gq/G11 Metastin 45-54, [125I]- agonist

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Leukotriene

Subtype G-protein coupling Species Radioligand Pharmacological action
BLT1 Gq/G11 Human Leukotriene B4, [3H]- endogenous
CysLT1 Gq/G11 Human Leukotriene D4, [3H]- endogenous
Leukotriene C4, [3H]- endogenous

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Melanin-concentrating hormone

Subtype G-protein coupling Radioligand Pharmacological action
MCH1 Gq/G11 MCH (Phe13, [125I]Tyr19) agonist
MCH (human), [125I]Tyr13- agonist
hMCH-1R Antagonist, [125I]- MCH1 antagonist
S36057, [125I]Tyr- antagonist
MCH2 Gq/G11 MCH (Phe13, [125I]Tyr19) agonist
MCH (human), [125I]Tyr13- agonist
MCH (Phe13, [125I]Tyr19) agonist
S36057, [125I]Tyr- antagonist

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Melanocortin

Subtype G-protein coupling Radioligand Pharmacological action
MC1 Gs NDP-MSH, [125I]Tyr2- MC1, MC3, MC4, M5 agonist
MT II, [125I]His- MC1, MC3, MC4, M5 agonist
SHU9119, [125I]- partial agonist
MC2 Gs ACTH (1-39), [125I]Tyr23- MC2 agonist
ACTH (1-39), [125I]Tyr2- MC2 agonist
MC3
MC4		 Gs NDP-MSH, [125I]Tyr2- MC1, MC3, MC4, M5 agonist
MT II, [125I]His- MC1, MC3, MC4, M5 agonist
AGRP (human), [125I]- inverse agonist
SHU9119, [125I]- antagonist
MC5 Gs NDP-MSH, [125I]Tyr2- MC1, MC3, MC4, M5 agonist
MT II, [125I]His- MC1, MC3, MC4, M5 agonist
AGRP (human), [125I]- inverse agonist
SHU9119, [125I]- partial agonist

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Melatonin

Subtype G-protein coupling Radioligand Pharmacological action
MT1
MT2		 Gi/G0 Melatonin, [O-methyl-3H]- endogenous
Melatonin, 2-[125I]- agonist

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Metabotropic glutamate

Subtype G-protein coupling Radioligand Pharmacological action
mGlu1 Gq/G11 Quisqualic acid,[3-3H(N)]- mGlu1, mGlu5 agonist
mGlu3 Gi/G0 NAAG, [glutamate-3,4-3H]- mGlu3 agonist
mGlu5 Gq/G11 Quisqualic acid,[3-3H(N)]- mGlu1, mGlu5 agonist
    Glutamic acid, L-[3,4-3H(N)]- endogenous

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Motilin

Subtype G-protein coupling Radioligand Pharmacological action
motilin Gq/G11 Motilin, [125I]- endogenous

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Muscarinic (see Acetylcholine)

Neurokinin (see Tachykinin)

Neuromedin U

Subtype G-protein coupling Radioligand Pharmacological action
NMU1 Gq/G11 NMU-25 (poucine), [125I]Tyr18- NMU1, NMU2 agonist
NMU-8 (poucine), [125I]Tyr1- NMU1, NMU2 agonist
NMU2   NMU-25 (poucine), [125I]Tyr18- NMU1, NMU2 agonist
NMU-8 (poucine), [125I]Tyr1- NMU1, NMU2 agonist

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Neuropeptide FF/neuropeptide AF

Subtype G-protein coupling Radioligand Pharmacological action
NPFF1
NPFF2		 Gi/G0 NPYFF (D-[125I]Tyr1, N-MePhe3) NPFF1, NPFF2 agonist

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Neuropeptide S

Subtype G-protein coupling Radioligand Pharmacological action
NPS GS NPS (human) ([125I]Tyr10) agonist

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Neuropeptide W/neuropeptide B

Subtype G-protein coupling Radioligand Pharmacological action
NPBW1 Gi/G0 des-Br-NPB-B23, [125I]- agonist
NPBW2 Gi/G0 NPW-23, [125I]- agonist

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Neuropeptide Y

Subtype G-protein coupling Radioligand Pharmacological action
Y1 Gi/Go PYY (human), [125I]- agonist
PYY (porcine), [125I]- Y1, Y4 agonist
PP (human), [125I]- agonist
Y2 Gi/Go PYY (human), [125I]- agonist
PYY (human) (Leu31, Pro34), [125I]- Y2, Y5 agonist
PP (human), [125I]- agonist
NPY (porcine), [125I]Bolton-Hunter labeled agonist
Y4 Gi/Go PYY (porcine), [125I]- Y1, Y4 agonist
Y5 Gi/Go PYY (human) (Leu31, Pro34), [125I]- Y2, Y5 agonist

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Neurotensin

Subtype G-protein coupling Radioligand Pharmacological action
NTS1
NTS2		 Gq/G11 Neurotensin, [125I]Tyr3- agonist
Neurotensin, [3,11-tyrosyl-3,5-3H(N)]- endogenous

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Opioid

Subtype G-protein coupling Radioligand Pharmacological action
delta Gi/Go Deltorphin II (D-Ala2), [tyrosyl-3,5-3H]- δ agonist
DPDPE, [tyrosyl-2,6-3H(N)]- δ agonist
DADLE, [tyrosyl-3,5-3H(N)]- δ, µ agonist
Diprenorphine [15,16-3H]- agonist
Naltrindole, [5',7'-3H]- antagonist
Naloxone, [N-allyl-2,3-3H]- antagonist
kappa Gi/Go U-69,593, [phenyl-3,4-3H]- κ agonist
DAMGO, [tyrosyl-3,5-3H(N)]- partial agonist
Diprenorphine, [15,16-3H]- antagonist
Naltrindole, [5',7'-3H]- antagonist
Naloxone, [N-allyl-2,3-3H]- antagonist
mu Gi/Go DADLE, [tyrosyl-3,5-3H(N)]- δ, µ agonist
DAMGO, [tyrosyl-3,5-3H(N)]- κ, µ agonist
Diprenorphine, [15,16-3H]- antagonist
Naltrindole, [5',7'-3H]- antagonist
Naloxone, [N-allyl-2,3-3H]- antagonist
NOP (ORL1) Gi/Go Nociceptin (Tyr14), [125I]- NOP agonist
Nociceptin, [leucyl-3,4,5-3H]- NOP agonist

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Orexin

Subtype G-protein coupling Radioligand Pharmacological action
OX1 Gi/G0
Gq/G11		 Orexin-A, [125I]- OX1, OX2 agonist
OX2 Gq/G11 Orexin-A, [125I]- OX1, OX2 agonist

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P2Y

Subtype G-protein coupling Radioligand Pharmacological action
P2Y1 Gq/G11 2MeSADP, [33P]- agonist
ADP, [3H]- agonist
P2Y2 Gq/G11 ATP, [3H]- agonist
UTP, [3H]- agonist
P2Y4 Gq/G11 UTP, [3H]- agonist
ATP, [3H]- antagonist
P2Y11 Gq/G11 ATPγS, [35S]- agonist
dATP, [3H]- agonist
NAD, [3H]- agonist
UTP, [3H]- agonist
P2Y12 Gq/G0 2MeSADP, [33P]- agonist
ADP, [3H]- agonist
ATP, [3H]- agonist
ATPγS, [35S]- agonist
P2Y13 Gi/G0 2MeSADP, [33P]- agonist
ADP, [3H]- agonist
ATP, [3H]- agonist
ATPγS, [35S]- agonist
P2Y14 Gi/G0 UDP-Glu, [glucose-6-3H]- agonist
UDP-GlcNAc, [galactosamin-6-3H]- agonist

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Parathyroid hormone

Subtype G-protein coupling Radioligand Pharmacological action
PTH1 GS PTH (1-34) amide (rat), (Nle8,21,[125I]Tyr34) PTH1, PTH2 agonist
PTH (1-34) (human), (Nle8,18, [125I]Tyr34)  

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Peptide P518

Subtype G-protein coupling Radioligand Pharmacological action
QRFP Gq/G11 QRFP-43, [125I]- QRFP, endogenous

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Platelet-activating factor

Subtype G-protein coupling Radioligand Pharmacological action
PAF Gq/G11 Hexadecyl-2-acetyl-sn-glyceryl-3-phosphorylcholine, 1-O-[acetyl-3H(N)]- endogenous

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Prokineticin

Subtype G-protein coupling Radioligand Pharmacological action
PKR1 Gq/G11 MIT-1, [125I]Bolton-Hunter labeled PKR1, PKR2 agonist
PKR2 Gi/G0
Gq/G11		 MIT-1, [125I]Bolton-Hunter labeled PKR1, PKR2 agonist

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Prostanoid

Subtype G-protein coupling Radioligand Pharmacological action
DP1 Gs Iloprost, [3H]- agonist
Prostaglandin D2, [3H]- endogenous
Prostaglandin E2, [3H]- endogenous
Prostaglandin F2α, [3H]- endogenous
DP2 Gi/G0 Prostaglandin D2, [3H]- endogenous
Prostaglandin E2, [3H]- endogenous
Prostaglandin F2α, [3H]- endogenous
EP1 Gq/G11 Iloprost, [3H]- agonist
Prostaglandin D2, [3H]- endogenous
Prostaglandin E2, [3H]- endogenous
Prostaglandin F2α, [3H]- endogenous
EP2 Gs Iloprost, [3H]- agonist
Prostaglandin D2, [3H]- endogenous
Prostaglandin E2, [3H]- endogenous
Prostaglandin F2α, [3H]- endogenous
EP3 Gi/G0 Iloprost, [3H]- agonist
Prostaglandin E2, [3H]- endogenous
Prostaglandin F2α, [3H]- endogenous
EP4 Gs Iloprost, [3H]- agonist
Prostaglandin D2, [3H]- endogenous
Prostaglandin E2, [3H]- endogenous
Prostaglandin F2α, [3H]- endogenous
FP Gq/G11 Iloprost, [3H]- agonist
Prostaglandin D2, [3H]- endogenous
Prostaglandin E2, [3H]- endogenous
Prostaglandin F2α, [3H]- endogenous
IP1 Gs Iloprost, [3H]- agonist
TP Gq/G11 Iloprost, [3H]- agonist
Prostaglandin E2, [3H]- endogenous
Prostaglandin F2α, [3H]- endogenous

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Relaxin family peptide

Subtype G-protein coupling Radioligand Pharmacological action
RXFP1 GS H2 Relaxin, [125I]Bolton-Hunter Labeled agonist
H3 Relaxin, [125I]Bolton-Hunter Labeled agonist
RXFP2 GS
Gi/Go		 H2 Relaxin, [125I]Bolton-Hunter Labeled agonist
H3 Relaxin, [125I]Bolton-Hunter Labeled agonist
INSL-3, [125I]- agonist
RXFP3 Gi/Go H3 Relaxin, [125I]Bolton-Hunter Labeled agonist
R3/ I5 (human chimera), [125I]- agonist
RXFP4 Gi/Go H3 Relaxin, [125I]Bolton-Hunter Labeled agonist
INSL-3, [125I]- agonist

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Somatostatin

Subtype G-protein coupling Radioligand Pharmacological action
sst1
sst2
sst3
sst4
sst5		 Gi/Go Somatostatin-14, ([125I]Tyr11) sst1-sst5 agonist
Somatostatin-14, ([125I]Tyr11) sst1-sst5 agonist
LTT-SRIF-28, ([125I]Tyr25) sst1-sst5 agonist
   

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Tachykinin

Subtype G-protein coupling Radioligand Pharmacological action
NK1 GS
Gq/G11		 Hemokinin-1, [125I]Bolton-Hunter labeled agonist
Neurokinin A, [125I]His1- agonist
Substance P, [leucyl-3,4,5-3H(N)]- agonist
Substance-P (Sar9, 11-Met(O2)), [2-prolyl-3,4-3H]- NK1 agonist
NK2 GS
Gq/G11		 Eledoisin (Lys4), [125I]Bolton-Hunter labeled NK2, NK3 agonist
Hemokinin-1, [125I]Bolton-Hunter labeled agonist
Neurokinin A, [125I]His1- agonist
Substance P, [leucyl-3,4,5-3H(N)]- agonist
SR 48968, [benzamide-4-3H]- NK2 antagonist
Neurokinin B (MePhe7), [125I]His3- NK2, NK3 agonist
NK3 Gq/G11 Eledoisin (Lys4), [125I]Bolton-Hunter labeled NK2, NK3 agonist
Hemokinin-1, [125I]Bolton-Hunter labeled agonist
Neurokinin A, [125I]His1- agonist
Neurokinin B (MePhe7), [125I]His3- NK2, NK3 agonist
Senktide, [phenylalanyl-3,4,5-3H]- NK3 agonist
SR142801, [3H] NK3 agonist

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Thyrotropin-releasing hormone

Subtype G-protein coupling Radioligand Pharmacological action
TRH1 Gq/G11 TRH (3-Methyl-histidine2), [3H]- agonist
TRH, [125I]His2- agonist

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Urotensin

Subtype G-protein coupling Radioligand Pharmacological action
UT Gq/G11 Urotensin II (human), [125I]Tyr9- Endogenous

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Vasoactive Intestinal Peptide

Subtype G-protein coupling Radioligand Pharmacological action
PAC1 Gs PACAP-27, [125I]- PAC1, endogenous
VPAC1 Gs VIP, [125I]- VPAC1, endogenous
VPAC2 Gs

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Vasopressin and Oxytocin

Subtype G-protein coupling Radioligand Pharmacological action
V1A Gq/G11 Vasopressin (linear), V1A antagonist, [125I]Tyr9- V1A antagonist
AVP, [phenylalanyl-3,4,5-3H(N)]- endogenous
Oxytocin, [tyrosyl-2,6-3H]-, endogenous
V1B Gq/G11 AVP, [phenylalanyl-3,4,5-3H(N)]- endogenous
Oxytocin, [tyrosyl-2,6-3H]-, endogenous
V2 Gs AVP, [phenylalanyl-3,4,5-3H(N)]- endogenous
Oxytocin, [tyrosyl-2,6-3H]-, endogenous
OT Gq/G11 Ornithine Vasotocin Analog, [125I]- antagonist
Oxytocin, [125I] Tyr2- endogenous
Oxytocin, [3H]-, endogenous

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Transporters すべて展開　|　すべて折り畳む

Acetylcholine

Radioligand Pharmacological action
Hemicholinium-3 diacetate salt, [methyl-3H]- Uptake inhibitor

Dopamine

Radioligand Pharmacological action
WIN 35428, [N-methyl-3H]- Uptake inhibitor
RTI-55, [125I]- Uptake inhibitor
RTI-121, [125I]- Uptake inhibitor
Mazindol, [4'-3H]- Uptake inhibitor
GBR 12935, [propylene-2,3-3H]- Uptake inhibitor
MPP(+), N-methyl-3H]- Uptake inhibitor

Norepinephrine

Radioligand Pharmacological action
Nisoxetine HCl, [N-methyl-3H]- Uptake inhibitor
Desmethylimipramine HCl, [benzene ring, 10,11-3H]- Uptake inhibitor

Serotonin

Radioligand Pharmacological action
Imipramine HCl, [benzene ring-3H(N)]- Uptake inhibitor
Paroxetine, [phenyl-6'-3H]- Uptake inhibitor
Citalopram, [N-methyl-3H]- Uptake inhibitor

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Ligand-gated ion channels すべて展開　|　すべて折り畳む

5-Hydroxytryptamine（5-HT3）

Radioligand Pharmacological action
GR 65630, [N-methyl-3H]- 5-HT3A antagonist
BRL-43694, [9-methyl-3H]- 5-HT3 blocker

Aspartate

Radioligand Pharmacological action
Aspartic acid, D-[2,3-3H]- endogenous

GABAA

Radioligand Pharmacological action
Diazepam, [methyl-3H]- agonist (BZ site)
Flunitrazepam, [methyl-3H]- agonist (BZ site)
Muscimol, [methylene-3H(N)]- agonist (GABA site )
SR 95531, [butyryl-2,3-3H]- antagonist (GABA site)
Pregnan-3α-ol-20-one, 5α- [9,11,12-3H(N)]- allosteric modulator
Ro 5-4864, [N-methyl-3H]- peripheral BZ agonist
PK 11195, [N-methyl-3H]- peripheral BZ antagonist
Ro 15-1788, [N-methyl-3H]- central BZ antagonist
Ro 15-4513, [7,9-3H]- partial agonist (BZ site)
TBOB, [3H]- antagonist
TBPS, [35S]- anion channel blocker

Glycine

Radioligand Pharmacological action
Glycine, [2-3H}- agonist
Taurine, [2-3H(N)]- agonist
Strychnine, [benzene ring-3H]- antagonist
Colchicine, [ring C, methoxy-3H]- α2 subunit inhibition

Ionotropic glutamate receptors

Radioligand Pharmacological action
Aspartic acid, D-[2,3-3H] NMDA agonist (glutamate site)
CGP 39653, [propyl-2,3,3H]- NMDA agonist (glutamate site)
Glycine, [2-3H]- NMDA agonist (glycine site)
Serine, D-[3H(G)]- NMDA agonist (glycine site)
MDL 105,519, [3H]- NMDA antagonist (glycine site)
MK-801, (+)-[3-3H]- non-competitive NMDA antagonist (ion channel site)
Ifenprodil, [phenyl-3H]- non-competitive NMDA antagonist (polyamine site)
AMPA, DL-α-[5-methyl-3H]- AMPA agonist
Kainic acid, [vinylidene-3H]- Kainate agonist
NAAG, [glutamate-3,4-3H]- endogenous
Glutamic Acid, L-[3,4-3H]- endogenous

Nicotinic acetylcholine

Radioligand Pharmacological action
Epibatidine, [125I]- CNS, skeletal muscle and autonomic ganglion activator
Epibatidine, (+/-)-[5,6-bicycloheptyl-3H]- CNS, skeletal muscle and autonomic ganglion activator
Choline chloride, [methyl-3H]-  
A-85380, [125I]- Neuronal CNS alpha4 beta2
α-Bungarotoxin, N-[propionyl-3H]propionylated Neuromuscular blocker
α-Bungarotoxin (Tyr54), [125I]- Neuromuscular blocker
Cytisine HCl, [3,5-3H(N)]- CNS activator
Nicotine, L-(-)-[N-ethyl-3H]- CNS activator

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Voltage-gated ion channels すべて展開　|　すべて折り畳む

Calcium Channel

Subtype Radioligand Pharmacological action
N-type ω-Conotoxin MVIIC, [125I]- anatgonist
ω-Conotoxin GVIA, [125I]Tyr22- antagonist
L-type Diltiazem, cis-(+)-[N-methyl-3H]- antagonist
Desmethoxyverapamil, (-)-[N-methyl-3H]- antagonist
Nitrendipine, [5-methyl-3H]- antagonist
PN200-110, (+)-[5-methyl-3H]- antagonist
Verapamil HCl, [N-methyl-3H]- antagonist
T-type Anandamide, [3H]- antagonist
Ryanodine Ryanodine, [9,21-3H(N)]- agonist
Calcium-45 Radionuclide  
- Gabapentin, [3H(G)]- Binds to voltage-sensitive Ca2+ channels

hERG (see Potassium Channels, Kv11.1)

Potassium Channels

Subtype Radioligand Pharmacological action
Calcium-Activated Apamin, [125I]His18-NH2 KCa2.1, KCa2.2, KCa2.3 antagonist
Inwardly Rectifying Arachidonic acid, [3H]- Kir2.3 agonist
Putrescine 2HCl, [1,4-3H(N)]- Kir2.3 agonist
Spermidine 3HCl, [3H]- Kir2.3 antagonist
Glibenclamide, [cyclohexyl-2,3-3H(N)]- Kir6.2 antagonist
Voltage-Gated α-Dendrotoxin, [125I]- KV1.6 pore blocker
PI(4,5)P2, [inositol-2-3H(N)]- KV7.1, KV7.2, KV7.3, KV7.4 activator
Dofetilide, [N-methyl-3H] KV10.1 pore blocker
Astemizole, [O-methyl-3H]- KV11.1 pore blocker
BeKm-1, [125I]Tyr11- KV11.1 gating inhibitor
Rubidium-86 Radionuclide  

Sodium Channel

Subtype Radioligand Pharmacological action
  Batrachotoxinin A 20-α-Benzoate, [benzoyl-2,5-3H]- activator
ProTX-II (tarantula), [125I]- NaV1.7 inhibitor
Sodium-22 Radionuclide  

Transient receptor potential

Subtype Radioligand Pharmacological action
TRPM2 Arachidonic acid, [3H]- agonist
TRPM4 PI(4,5)P2, [inositol-2-3H(N)]- agonist
ADP, [3H]- antagonist
Spermidine 3HCl, [3H]- antagonist
TRPV1 Resiniferatoxin, [125I]- pore blocker

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Nuclear receptors すべて展開　|　すべて折り畳む

Estrogen receptor

Subtype Complementary radioligands Pharmacological action
ER-α/-β
(NR3A1/NR3A2)		 Estradiol, [2,4,6,7,16,17-3H(N)]- agonist
Estradiol, [2,4,6,7-3H(N)]- agonist
Estrone, [2,4,6,7-3H]- agonist

3-Ketosteroid receptors

Subtype Complementary radioligands Pharmacological action
GR (NR3C1) Dexamethasone, [1,2,6,7-3H(N)]- agonist
Corticosterone, [1,2,6,7-3H(N)]- agonist
Hydrocortisone [1,2,6,7-3H(N)]- agonist
MR (NR3C2) Aldosterone, D-[1,2,6,7-3H(N)]- agonist
Dexamethasone, [1,2,6,7-3H(N)]- agonist
Hydrocortisone [1,2,6,7-3H(N)]- agonist
Progesterone, [1,2,6,7-3H(N)]- agonist
PR (NR3C3) Progesterone, [1,2,6,7-3H(N)]- agonist
Promegestone (R5020), [17α-methyl-3H]- photoaffinity agonist
AR (NR3C4) Androst-4-ene-3,17-dione, [1,2,6,7-3H(N)]- agonist
Dihydrotestosterone, [1,2,4,5,6,7-3H(N)]- agonist
Testosterone, [1,2,6,7,16,17-3H(N)]- agonist
Testosterone, [1,2,6,7-3H(N)]- agonist
Methyltrienolone (R1881), [17α-methyl-3H]- agonist
Mibolerone, [17α-methyl-3H]- agonist

Thyroid hormones

Subtype Complementary radioligands Pharmacological action
TR-α/-β
(NR1A1/NR1A2)		 T4, [125I]- agonist
T4, [125I]- agonist
T3, [125I]- agonist
T3, [125I]- agonist
Reverse T3, [125I]- agonist

Vitamin D receptor-like

Subtype Complementary radioligands Pharmacological action
VDR (NR1I1) 1α, 25-(OH)2 D3, [26,27-3H]- agonist
PXR (NR1I2) Dexamethasone, [1,2,4,6,7-3H(N)]- agonist

Liver X receptor-like

Subtype Complementary radioligands Pharmacological action
LXR-α/-β
(NR1H3/ NR1H2) 		24(S),25-Epoxycholesterol, [26,27-3H]- agonist

Retinoic acid receptors

Subtype Complementary radioligands Pharmacological action
NR1B1/ NR1B2/ NR1B3 9-cis-Retinoic acid, [11,12-3H]- agonist
all-trans-Retinoic acid, [11,12-3H]- agonist

 

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