標識リガンド一覧

GPCR、トランスポーターやチャンネルの区分は、IUPHAR/BPS Guide to Pharmacology を参考にしています。

GPCRs:  数字 | A | B | C | D | E | G | H | L | M | N | O | P | Q | R | S | T | V
Transporters
Voltage-gated ion channels
Ligand-gated ion channels
Nuclear hormone receptors

 


GPCRs すべて展開 | すべて折り畳む

5-Hydroxytryptamine (Serotonin) receptor

Subtype Raioligands Pharmacological action (human) Code
  5-Hydroxytryptamine creatinine sulfate, [1,2-3H(N)]- endogenous NET498
5-Hydroxytryptamine, [3H(G)]- endogenous NET1167
5-HT1 5-CT, [3H]- 5-HT1A,1B, 1D, 5a, 7 agonist NET1188
GR125743, [N-methyl-3H]- 5-HT1B, 1D antagonist NET1172
WAY100635 [methoxy-3H] 5-HT1A antagonist NET1164
5-HT2 (±)-DOI, [125I]- 5-HT2C agonist NEX255
Ketanserin HCl, [ethylene-3H]- 5-HT2A antagonist NET791
Mesulergine, [N-methyl-3H]- 5-HT2C inverse agonist NET1148
N-Methylspiperone, [N-methyl-3H]- rat 5-HT2A antagonist NET856
5-HT3  (ligand-gated ion channel) see Ion Channels
5-HT4 GR113808, [N-methyl-3H]- 5-HT4 antagonist NET1152
5-ht5a 5-CT, [3H]- 5-HT1A,1B, 1D, 5a, 7 agonist NET1188
Iodo-LSD, [125I]- 5-ht5a agonist NEX199
5-HT6 SB-258585, [125I]- 5-HT6 antagonist NEX424
5-HT7 5-CT, [3H]- 5-HT1A,1B, 1D, 5a, 7 agonist NET1188
SB-269970, [3H]- 5-HT7 antagonist NET1198

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Acetylcholine (Muscarinic) receptor

Subtype Radioligands Pharmacological action (human) Code

Acetylcholine iodide, [acetyl-3H]- endogenous NET113

AF-DX 384, [2, 3-dipropylamino-3H]- M2, M4 antagonist NET1041
  4-DAMP, [N-methyl-3H]- M1-M5 antagonist NET1040
  Oxotremorine-M acetate, [methyl-3H]- M1-M4 agonist NET671 
  Pirenzepine, [N-methyl-3H]- M1 antagonist NET780
  Scopolamine methyl chloride (NMS), [N-methyl-3H]- M1-M5 antagonist NET636

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Adenosine receptor

Subtype Radioligands Pharmacological action (human) Code

Adenosine, [2,8-3H]- endogenous NET063
  AB-MECA, [125I]- A3 agonist NEX312
  CGS 21680, [carboxyethyl-3H(N)]- A2A agonist NET1021
  NECA, [adenine-2,8-3H]- A1, A2A, A3 agonist NET811

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Adrenoceptor

Subtype Radioligands Pharmacological action (human) Code

Norepinephrine, levo-[ring-2,5,6-3H]- endogenous NET678
α1 Ketanserin HCl, [ethylene-3H]- α1A, 1B,1D antagonist NET791
Prazosin, [7-methoxy-3H]- α1A, 1B, 1D inverse agonist, α2c antagonist NET823
α2 MK-912, [3H(G)]- α2A, 2B, 2C antagonist NET1227
RX821002, [6,7-3H]- α2A, 2B, 2C antagonist NET1153
β (-)-CGP 12177, [5,7-3H]- β1 antagonist NET1061
(-)-Cyanopindolol, [125I]- β1 antagonist NEX189
(±)-Cyanopindolol, [125I]- β1, β2 antagonist, β3 partial agonist NEX174
Propranolol, L-(-)-[4-3H]- β1 antagonist NET515

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Angiotensin receptor

Subtype Radioligands Pharmacological action (human) Code
  Angiotensin II, [125I]Tyr4- AT1, AT2 agonist  NEX105
  Angiotensin II (Sar1, Ile8), [125I]Tyr4 AT1 antagonist NEX248
  CGP42112A, [125I]- AT2 agonist NEX324

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Apelin receptor

Subtype Radioligands Pharmacological action (human) Code
Aperin Apelin 13 (Glp65, Nle75, [125I]Tyr77) agonist NEX393

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Bombesin receptor

Subtype Radioligands Pharmacological action (human) Code

Bombesin, [125I]Tyr4- BB1, BB2, BB3 agonist NEX258
  Bombesin (6-14) (D-[125I]Tyr6- βAla11, Phe13, Nle14) BB3 agonist NEX377

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Bradykinin receptor

Subtype Radioligands Pharmacological action (human) Code
  Bradykinin, [2,3-prolyl-3,4-3H]- endogenous NET706

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Calcitonin receptor

Subtype Radioligands Pharmacological action (human) Code
CT Calcitonin (salmon), [125I]Tyr22- agonist NEX423

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Cannabinoid receptor

Subtype Radioligands Pharmacological action (human) Code
  CP 55940, [side chain-2,3,4-3H(N)]- CB1, CB2 agonist NET1051
  SR141716A, [3H] CB1 antagonist NET1158

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Chemokine receptor

Subtype Radioligands Pharmacological action (human) Code
CCR1 MCP-1 (CCL2), [125I]Bolton-Hunter labeled CCR1, CCR2 agonist NEX332
MIP-1α (CCL3), [125I]- CCR1, CCR5 agonist NEX298
CCR2 Eotaxin (CCL11), [125I]- CCR2, CCR3, CCR5 agonist NEX314
MCP-1 (CCL2), [125I]Bolton-Hunter labeled CCR1, CCR2 agonist NEX332
CCR3 Eotaxin (CCL11), [125I]- CCR2, CCR3, CCR5 agonist NEX314
CCR5 MIP-1α (CCL3), [125I]- CCR1, CCR5 agonist NEX298
CXCR3 IP-10 (CXCL10), [125I]Bolton-Hunter labeled CXCR3 agonist NEX348
CXCR4 SDF-1α (CXCL12α), [125I]- CXCR4, ACKR3 agonist NEX346
CX3CR1 Fractalkine (CX3CL1), [125I]- CX3XR1 agonist NEX368
ACKR3 SDF-1α (CXCL12α), [125I]- CXCR4, ACKR3 agonist NEX346

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Cholecystokinin receptor

Subtype Radioligands Pharmacological action (human) Code

CCK-8, [125I]Bolton-Hunter labeled CCK1, CCK2 agonist NEX203
  CCK-8, [3H]propionylated CCK1, CCK2 agonist NET1162
  Gastrin I, [125I]Tyr12- CCK2 agonist NEX176

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Corticotropin-releasing factor receptor

Subtype Radioligands Pharmacological action (human) Code
  CRF (human, rat), [125I]Tyr0- CRF1 agonist NEX216
  CRF (ovine), [125I]Tyr0- CRF1 agonist NEX217
  Sauvagine, [125I]Tyr0- CRF1, CRF2 agonist NEX306

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Dopamine receptor

Subtype Radioligands Pharmacological action (human) Code

3,4-Dihydroxyphenylethylamine, [3H(G)]- endogenous NET1160
3,4-Dihydroxyphenylethylamine, [ring-2,5,6-3H]- endogenous NET673
3,4-Dihydroxyphenylethylamine, [7-3H]- endogenous NET131
D1 SCH 23390, [N-methyl-3H]- D1, D5 antagonist NET930
D2 7-OH-DPAT, R-(+)-[3H]- D2, D3 agonist NET1169
Methylspiperone, [N-methyl-3H]- rat D2, D4 antagonist NET856
Raclopride, [methoxy-3H]-  rat D2 antagonist NET975
D3 7-OH-DPAT, R-(+)-[3H]- D2, D3 agonist NET1169
YM-09151-2 (Nemonapride), [N-methyl-3H]-  D3, D4 antagonist NET1004
D4 YM-09151-2 (Nemonapride), [N-methyl-3H]-  D3, D4 antagonist NET1004
Methylspiperone, [N-methyl-3H]- rat D2, D4 antagonist NET856
D5 SCH 23390, [N-methyl-3H]- D1, D5 antagonist NET930

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Endothelin receptor

Subtype Radioligands Pharmacological action (human) Code

Endothelin-1, [125I]Tyr13- ETA, ETB agonist NEX259

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Estrogen (G protein-coupled) receptor

Subtype Radioligands Pharmacological action (human) Code
GPER Estradiol, [2,4,6,7,16,17-3H(N)]- endogenouse NET517
Estradiol, [2,4,6,7-3H(N)]- endogenouse NET317
Estradiol, [6,7-3H(N)]- endogenouse NET013

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GABAB receptor

Subtype Radioligands Pharmacological action (human) Code

GABA, [2,3-3H(N)]- endogenous NET191X
GABAA (ligand-gated ion channel) see Ion Channels

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Ghrelin receptor

Subtype Radioligands Pharmacological action (human) Code

Ghrelin (human), [125I]His9- agonist NEX388

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Glucagon receptor family

Subtype Radioligands Pharmacological action (human) Code
GIP GIP (human), [125I]- agonist NEX402
GLP-1 GLP-1 (7-36) amide, [125I]Tyr13- agonist NEX308
glucagon Glucagon, [125I]- agonist NEX207

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Gonadotrophin-releasing hormone receptor

Subtype Radioligands Pharmacological action (human) Code
GnRH LH-RH (D-Trp6), [125I]Tyr5-
NEX365

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Histamine receptor

Subtype Radioligands Pharmacological action (human) Code

Histamine 2HCl, [ring, methylenes-3H(N)]- endogenous NET732
H1 Astemizole, [O-methyl-3H]- H1 antagonist NET1140
Pyrilamine, [pyridinyl 5-3H]- H1 inverse agonist NET594
H2 Iodoaminopotentidine, [125I]- rat H2 antagonist NEX431
H3 Iodoproxifan, [125I]- H3 antagonist NEX436

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Hydroxycarboxylic acid receptor

Subtype Radioligands Pharmacological action (human) Code
HCA2 Nicotinic acid, [3H(G)]- agonist NET1230

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Lysophospholipid receptor

Subtype Radioligands Pharmacological action (human) Code
LPA Lysophosphatidic acid, 1-[9,10-3H(N)]oleoyl- endogenous NET1100
S1P Sphingosine 1-phosphate, [33P]- endogenous NEG381H

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Melanin-concentrating hormone receptor

Subtype Radioligands Pharmacological action (human) Code
  S36057, [125I]Tyr- MCH1 antagonist NEX396

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Melanocortin receptor

Subtype Radioligands Pharmacological action (human) Code

ACTH (1-39), [125I]Tyr23 - MC2 agonist NEX165
  NDP-MSH, [125I]Tyr2- MC1, MC3, MC4, MC5 agonist NEX352
  SHU9119, [125I]- MC1, MC5 partal agonist, MC3, MC4 antagonist NEX362

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Melatonin receptor

Subtype Radioligands Pharmacological action (human) Code

Melatonin, [O-methyl-3H]- endogenous NET801
  Melatonin, 2-[125I]iodo- MT1, MT2 agonist NEX236

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Metabotropic glutamate receptor

Subtype Radioligands Pharmacological action (human) Code

Glutamic acid, L-[3,4-3H]- endogenous NET490
  NAAG, [glutamine-3,4-3H]- endogenous NET1082
  Quisqualic acid, [3H] rat mGlu1, mGlu5 agonist NET1165

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Motilin receptor

Subtype Radioligands Pharmacological action (human) Code

Motillin (human), [125I]Tyr0- agonist NEX378

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Neuropeptide Y receptor

Subtype Radioligands Pharmacological action (human) Code

PP (human), [125I]- agonist NEX315
  PYY (human), [125I]- Y1, Y2, Y5, Y6 agonist NEX341
  PYY (porcine), [125I]- Y1, Y4 agonist NEX240

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Neurotensin receptor

Subtype Radioligands Pharmacological action (human) Code

Neurotensin, [3,11-tyrosyl-3,5-3H(N)]- endogenous NET605
  Neurotensin, [125I]Tyr3- NTS1, NTS2 agonist NEX198

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Opioid receptor

Subtype Radioligands Pharmacological action (human) Code
δ DADLE, [tyrosyl-3,5-3H(N)]- δ, μ agonist NET648
Deltorphin II (D-Ala2), [tyrosyl-3,5-3H]- δ agonist NET1087
Diprenorphine, [15,16-3H]- δ agonist NET1121
DPDPE, [tyrosyl-2,6-3H(N)]- δ agonist NET922
κ U-69,593, [phenyl-3,4-3H]- κ agonist NET952
Diprenorphine, [15,16-3H]- κ antagonist NET1121
μ DADLE, [tyrosyl-3,5-3H(N)]- δ, μ agonist NET648
Naloxone, [N-allyl-2,3-3H]- μ antagonist NET719

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Orexin receptor

Subtype Radioligands Pharmacological action (human) Code

Orexin-A, [125I]- agonist NEX367

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P2Y receptor

Subtype Radioligands Pharmacological action (human) Code

ADP, [2,8-3H]- endogenous NET241
  ATP, [2,5',8-3H(N)]- endogenous NET1189
  UDP-Glu, [glucose-6-3H(N)]- endogenous NET1163
  2MeSADP, [33P]- PY13 agonist NEG380H

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Platelet-activating factor receptor

Subtype Radioligands Pharmacological action (human) Code

Hexadecyl PAF, 1-O-[acetyl-3H(N)]- endogenous NET910

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Prostanoid receptor

Subtype Radioligands Pharmacological action (human) Code
  Prostaglandin E2, [5,6,8,11,12,14,15-3H(N)]- endogenous NET428
  Prostaglandin F2α, [5,6,8,9,11,12,14,15-3H(N)]- endogenous NET433

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QRFP receptor

Subtype Radioligands Pharmacological action (human) Code
QRFP QRFP-43 (human), [125I]- agonist NEX408

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Relaxin family peptide receptor

Subtype Radioligands Pharmacological action (human) Code

INSL-3, [125I]- RXFP2 agonist NEX419

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Serotonin (see 5-Hydroxytryptamine)

Somatostatin

Subtype Radioligands Pharmacological action (human) Code
  Somatostatin-14, [125I]Tyr11- sst4, sst5 agonist NEX446

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Tachykinin receptor

Subtype Radioligands Pharmacological action (human) Code
NK1 Substance P, [125I]Tyr8- NK1 agonist NEX152
Substance-P (Sar9, 11-Met(O2)), [2-prolyl-3,4-3H]- NK1 agonist NET1025
NK2 Neurokinin A, [125I]His1- NK2 agonist NEX252
NK3 Neurokinin B (MePhe7), [125I]His3- NK3 agonist NEX285

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Thyrotropin-releasing hormone receptor

Subtype Radioligands Pharmacological action (human) Code

TRH(His(3-Me)2), [L-histidyl-4-3H(N), L-prolyl-3,4-3H(N)]-
NET705

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Vasopressin and oxytocin receptor

Subtype Radioligands Pharmacological action (human) Code

AVP, [phenylalanyl-3,4,5-3H(N)]- endogenous NET800
V1 Vasopressin (linear), V1A antagonist
(Phaa1, D-Tyr(Me)2, Arg6,8, [125I]Tyr9)
V1A antagonist NEX310
OT Ornithine Vasotocin Analog, [125I]- antagonist NEX254
Oxytocin, [125I]Tyr2-   NEX187

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VIP and PACAP receptor

Subtype Radioligands Pharmacological action (human) Code

PACAP-27 amide, [125I]- PAC1 agonist NEX294
  VIP, [125I]- VPAC1, VPAC2 agonist NEX192

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Transporters すべて展開 | すべて折り畳む

Chloline (CHT/SLC5A7)

Subtype Radioligands Pharmacological action (human) Code

Hemicholinium-3 diacetate salt, [methyl-3H]-
NET884

Monoamine Transportor

Subtype Radioligands Pharmacological action (human) Code
SLC6A2/ NET Mazindol, [4'-3H]- inhibition NET816
MPP+, [N-methyl-3H]- substrate NET914
RTI-55, [125I]- ligand NEX272
SLC6A3/ DAT GBR 12935, [propylene-2,3-3H]- inhibition NET918
Mazindol, [4'-3H]- inhibition NET816
MPP+, [N-methyl-3H]- substrate NET914
RTI-55, [125I]- ligand NEX272
WIN 35,428, [N-methyl-3H]- inhibition NET1033
SLC6A4/ SERT Citalopram, [N-methyl-3H]- inhibition NET1039
Escitalopram. [N-methyl-3H]- inhibition NET1209
Imipramine HCl, [benzene ring-3H(N)]- inhibition NET576
Paroxetine, [phenyl-6'-3H]- inhibition NET869
RTI-55, [125I]- ligand NEX272

Equilibrative nucleoside transporter 1 (SLC29A1)

Subtype Radioligands Pharmacological action (human) Code

NBTI, [3H]-
NET1213

Steroid-derived molecule transporter (SLC51)

Subtype Radioligands Pharmacological action (human) Code

Dehydroepiandrosterone sulfate, Na salt,
[1,2,6,7-3H(N)]-
substrate NET860
  Estrone sulfate, annonium salt, [6,7-3H(N)]- substrate NET203
  Taurocholic acid, [3H(G)]- substrate NET322

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

Potassium channels

Subtype Radioligands Pharmacological action (human) Code
Calcium-activated
potassium channel
Apamin, [125I]His18-NH2- KCa2.1, KCa2.2, KCa2.3 antagonist NEX242
Voltage-gated
potassium channel
Rubidium-86 Radionuclide   NEZ072 
Astemizole, [O-methyl-3H]- KV10.1, KV11.1 inhibition NET1140 
α-Dendrotoxin, [125I]- KV1.6 blocker NEX434 
Dofetilide, [N-methyl-3H] KV11.1 inhibition NET1144 

Voltage-gated calcium channel

Subtype Radioligands Pharmacological action (human) Code

Calcium-45 Radionuclide
NEZ013
  Nitrendipine, [5-methyl-3H]- CaV1.3 inhibition NET741
  Verapamil HCl, [N-methyl-3H]- CaV1.1, CaV1.2, CaV1.3 antagonist NET810
  Gabapentin, [3H(G)]- α2–δ1 subunits ligand NET1182
  ω-Conotoxin GVIA, [125I]Tyr22- rat CaV2.1, CaV2.2 antagonist NEX239
  ω-Conotoxin MVIIC, [125I]- rat CaV2.1, CaV2.2 antagonist NEX323

Voltage-gated sodium channel

Subtype Radioligands Pharmacological action (human) Code

Sodium-22 Radionuclide
NEZ081
  Batrachotoxinin A 20-α-Benzoate, [benzoyl-2,5-3H]- activator NET876
  ProTx-II, [125I]- Nav1.7 blocker NEX450

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

5-HT3 receptor

Subtype Radioligands Pharmacological action (human) Code
  GR 65630, [N-methyl-3H]- 5-HT3A antagonist NET1011

GABAA receptor

Subtype Radioligands Pharmacological action (human) Code

GABA, [2,3-3H]- endogenous NET191X
  Flunitrazepam, [methyl-3H]- α1, α2, α3, α5 allosteric modulator NET567
  Muscimol, [methylene-3H(N)]- agonist NET574
  SR 95531 (Gabazine), [butyryl-2,3-3H]- antagonist NET946
  Ro15-1788 (Flumazenil), [N-methyl-3H]- Allosteric modulator NET757
  Ro15-4513, [7,9-3H]- Allosteric modulator NET925
  TBPS, [35S]- chloride channel blocker NEG049

Glycine receptor

Subtype Radioligands Pharmacological action (human) Code

Glycine, [2-3H]- endogenous NET004
  Strychnine, [benzene ring-3H]- antagonist NET773
  Taurine, [2,3-3H]- agonist NET1205

Ionotropic glutamate receptor

Subtype Radioligands Pharmacological action (human) Code

Glutamic acid, L-[3,4-3H]- endogenouse NET490
  AMPA, DL-α-[5-methyl-3H]- agonist NET833
  Aspartic acid, D-[2,3-3H]- glutamine site agonist NET581
  Aspartic acid, L-[2,3-3H(N)]- glutamine site agonist NET390V
  CGP 39653, [propyl-2,3,3H]- glutamate site antagonist NET1050
  Glycine, [2-3H]- glycine site agonist NET004
  Kainic acid, [vinylidene-3H]- agonist NET875
  MDL 105,519, [3H]- glycine site antagonist NET1171
  MK-801, (+)-[3-3H]- Channel blocker/ NET972

Nicotinic acetylcholine receptor

Subtype Radioligands Pharmacological action (human) Code

Acetylcholine iodide, [acetyl-3H]- endogenous NET113
  α-Bungarotoxin, [125I]Tyr54- antagonist NEX126
  α-Bungarotoxin, [125I]- antagonist NEX126H
  α-Bungarotoxin, N-[3H]prppionylated antagonist NET1170
  Cytisine HCl, [3,5-3H(N)]- α2, α3, α4 agonist NET1054
  Epibatidine, [125I]- α2, α3, α4 agonist NEX358
  Epibatidine, (+/-)-[5,6-bicycloheptyl-3H]- α2, α3, α4, α7 agonist NET1102
  Nicotine, L-(-)-[N-methyl-3H]- antagonist NET827
Nuclear hormone receptors すべて展開 | すべて折り畳む

Estrogen receptor

Subtype Radioligands Pharmacological action (human) Code

Estradiol, [2,4,6,7,16,17-3H(N)]- endogenouse NET517
  Estradiol, [2,4,6,7-3H(N)]- endogenouse NET317
  Estradiol, [6,7-3H(N)]- endogenouse NET013

3-Ketosteroid receptor

Subtype Radioligands Pharmacological action (human) Code
Androgen
receptor / NR3C4
Dihydrotestosterone, [1,2,4,5,6,7-3H(N)]- endogenouse NET453
Testosterone, [1,2,6,7,16,17-3H(N)]- endogenouse NET553
Testosterone, [1,2,6,7-3H(N)]- endogenouse NET370
Mibolerone, [17α-methyl-3H]- agonist NET919
Glucocorticoid
receptor / NR3C1
Aldosterone, D-[1,2,6,7-3H(N)]- endogenouse NET419
Corticosterone, [1,2,6,7-3H(N)]- endogenouse NET399
Hydroxycortisone (Cortisol), [1,2,6,7-3H(N)]- endogenous NET396
Dexamethasone, [1,2,6,7-3H(N)]- agonist NET1192
Mineralocorticoid
receptor / NR3C2
Aldosterone, D-[1,2,6,7-3H(N)]- endogenous NET419
Corticosterone, [1,2,6,7-3H(N)]- endogenous NET399
Hydroxycortisone (Cortisol), [1,2,6,7-3H(N)]- endogenous NET396
Progesterone, [1,2,6,7-3H(N)]- endogenous NET381
Dexamethasone, [1,2,6,7-3H(N)]- agonist  NET1192
Progesterone
receptor / NR3C3
Progesterone, [1,2,6,7-3H(N)]- endogenous NET381

Thyroid Hormone Receptors

Subtype Radioligands Pharmacological action (human) Code

T3, L-[3'-125I]- agonist NEX110X
  T3, L-[3'-125I]- agonist NEX110H
  T4, L-[3',5'-125I]- agonist NET111X
  T4, L-[5'-125I]- agonist NET111H

Vitamin D receptor-like receptor

Subtype Radioligands Pharmacological action (human) Code
VDR (NR1I1) 1α, 25-(OH)2 D3, [26,27-3H]- endogenous NET626

Peroxisome proliferator-activated receptors

Subtype  Radioligands Pharmacological action (human)
Code
 PPAPγ (NR1C3)
 Rosiglitazone, D,L-[3H]-
 agonist  NET1143

Retinoic acid receptor

Subtype Radioligands Pharmacological action (human) Code

9-cis-Retinoic acid (Alitretinoin), [11,12-3H]- agonist NET1151