Radioligand | Nonspecific Binding | Tissue | Ki | |
---|---|---|---|---|
σ Receptors | ||||
σ1 | 5 nM [3H](+)-Pentazocine | 10 μM Haloperidol | Rat brain | 1.3 ± 0.4 |
σ2 | 3 nM [3H]Di-o-tolylguanidine | 10 μM Haloperidol | Rat brain | 0.6 ± 0.1 |
Monoamine transporters | ||||
Dopamine | 0.5 nM [3H]WIN 35,428 | 50 μM Cocaine | Rat striatum | 1175 ± 100 |
Serotonin | 0.2 nM [3H]Paroxetine | 1.5 μM Imipramine | Rat brainstem | 1402 ± 152 |
Norepinephrine | 0.5 nM [3H]Nisoxetine | 4 μM Desipramine | Rat cerebral cortex | >10,000 |
Other neurotransmitter receptors | ||||
Adenosine | 4.0 nM [3H]5′-N-Ethylcarboxamidoadenosine | 1 μM 5′-N-Ethylcarboxamidoadenosine | Bovine striatum | >10,000a |
Adrenergic, α1 | 0.3 nM [3H]7-MeOxy-prazosin | 1 μM Phentolamine | Rat forebrain | 695a |
Adrenergic, α2 | 1 nM [3H]RX 821002 | 1 μM Phentolamine | Rat cerebral cortex | >10,000a |
Adrenergic, β1 | 0.04 nM [125I](−)-Iodocyanopindolol | 3 μM Alprenolol | Human neuroepithelioma | >10,000a |
Cannabinoid, CB1 | 0.5 nM [3H]CP 55940 | 1 μM HU-210 | Human recombinant embryonic kidney 293 cells | >10,000a |
Cannabinoid, CB2 | 0.5 nM [3H]CP 55940 | 1 μM HU-210 | Human recombinant CHO cells | >10,000a |
Dopamine, nonselective | 0.3 nM [3H]Spiperone | 1 μM Spiperone | Bovine striatum | >10,000a |
Dopamine D1 | 0.18 nM [3H]SCH 23390 | 1 μM SCH 23390 | LHD1 cells | >10,000a |
Dopamine D2 | 5 nM [3H](−)-Sulpiride | 1 μM Haloperidol | Rat brain | 1041 ± 9 |
0.21 nM [3H]YM-09151-2 | 1 μM Chlorpromazine | CHOp cells | >10,000a | |
Dopamine D3 | 0.21 nM [3H]YM-09151-2 | 1 μM Chlorpromazine | CHOp cells | >10,000a |
Dopamine D4.2 | 0.15 nM [3H]Spiperone | 1 μM Haloperidol | Human recombinant CHO-K1 cells | 53a |
GABAA, agonist site | 5 nM [3H]GABA | 1 μM GABA | Bovine cerebellum | >10,000a |
GABAA, benzodiazepine α1 | 1 nM [3H]Flunitrazepam | 0.5 μM Flumazenil | Bovine cortex | >10,000a |
GABAB | 1 nM [3H]CGP 54626A | 100 μM Baclofen | Rat cerebral cortex | >10,000a |
Glutamate, AMPA | 5 nM [3H]AMPA | 100 μM AMPA | Rat forebrain | >10,000a |
Glutamate, kainate | 10 nM [3H]Kainic acid | 10 μM Kainic acid | Rat forebrain | >10,000a |
Glutamate, NMDA agonist | 2 nM [3H]CGP 39653 | 300 μM NMDA | Rat forebrain | >10,000a |
Glutamate, NMDA glycine | 4 nM [3H]MDL-105,519 | 3 μM MDL-105,519 | Rat cortex/hippoc | >10,000a |
Glutamate, NMDA/phencyclidine | 10 nM [3H]TCP | 100 μM (+)-MK801 | Rat forebrain | >10,000a |
5 nM [3H]TCP | 10 μM Cyclazocine | Rat brain | >10,000 | |
Glutamate, mGluR1 | 20 nM [3H]Quisqualic acid | 1 mM l-Glutamate | Rat cerebellum | >10,000a |
Glutamate, mGluR5 | 10 nM [3H]2-Methyl-6-(phenylethynyl)pyridine | 10 μM 2-Methyl-6-(phenylethynyl)pyridine | Rat brain | >10,000a |
Glycine, strychnine | 16 nM [3H]Strychnine | 100 μM Strychnine nitrate | Rat spinal cord | >10,000a |
Histamine H1 | 2 nM [3H]Pyrilamine | 10 μM Triprolidine | Bovine cerebellum | 853a |
Histamine H2 | 0.1 nM [125I]aminopotentidine | 3 μM Tiotidine | Guinea pig striatum | 2570a |
Histamine H3 | 0.2 nM [3H]N-α-Methylhistamine | 0.1 nM R-(−)-α-Methylhistamine | Rat forebrain | 2385a |
Melatonin | 70 pM [125I]2-Iodomelatonin | 0.1 μM 2-Iodomelatonin | Chicken brain | >10,000a |
Muscarinic, central | 0.15 nM [3H]Quinuclidinyl benzilate | 0.1 μM Atropine | Rat cerebral cortex | 3080a |
Muscarinic, peripheral | 0.3 nM [3H]Quinuclidinyl benzilate | 0.1 μM Atropine | Guinea pig bladder | 2155a |
Muscarinic, M1 | 0.5 nM [3H]N-Methyl scopolamine | 1 μM (−)-Scopolamine | Human recombinant CHO cells | >10,000a |
Muscarinic, M2 | 0.5 nM [3H]N-Methyl scopolamine | 1 μM Methylscopolamine | Human recombinant CHO cells | 1210a |
Nicotinic, muscle | 1 nM 125I-α-Bungarotoxin | 10 μM Nicotine | Human TE671 cells | >10,000a |
Nicotinic, neuronal | 0.05 nM [3H]Epibatidine | 20 nM Epibatidine | Human SK-N-F1 cells | >10,000a |
Opioid, nonselective | 0.5 nM [3H]Bremazocine | 10 μM Levallorphan | Rat brain | >10,000 |
1 nM [3H]Naloxone | 1 μM Naloxone | Rat forebrain | >10,000a | |
Serotonin, nonselective | 5 nM [3H]Lysergic acid diethylamide | 10 μM Methysergide | Rat cerebral cortex | 2060a |
5-HT1A | 0.50 nM [3H]8-Hydroxy-2-dipropylaminotetralin | 1 μM Dihydroergotamine | HA7 cells | 4985 ± 330a |
5-HT2 | 2 nM [3H]Ketanserin | 1 μM Mianserin | Rat brain | 1376 ± 159 |
5-HT2A | 0.40 nM [3H]Ketanserin | 1 μM Ketanserin | NIH-3T3-GF6 cells | 1129 ± 49a |
5-HT2C | 0.40 nM [3H]Mesulergine | 10 μM Mesulergine | NIH-3T3-Po cells | >10,000a |
Hormones, peptides, steroids | ||||
Angiotensin II, AT1 | 0.06 nM [125I](Sar1-Ile8)angiotensin | 1 μM Angiotensin II | Human KAN-TS cells | >10,000a |
Angiotensin II, AT2 | 0.1 nM [125I]Tyr4-angiotensin II | 0.05 μM Angiotensin II | Bovine cerebellum | >10,000a |
Bradykinin, BK2 | 0.2 nM [3H]Bradykinin | 100 nM Bradykinin trifluoroacetic acid | Guinea pig ileum | >10,000a |
Cholecystokinin, CCKA | 0.02 nM [125I]CCK-8 | 1 μM CCK-8 | Mouse pancreas | >10,000a |
Cholecystokinin, CCKB | 0.02 nM [125I]CCK-8 | 1 μM CCK-8 | Mouse forebrain | >10,000a |
CRF, nonselective | 0.1 nM [125I]Tyr0-oCRF | 1 μM Tyr0-oCRF | Rat cerebral cortex | >10,000a |
Endothelin, ETA | 0.033 nM 125I-Endothelin-1 | 0.1 μM Endothelin-1 | Human neuroblastoma | >10,000a |
Endothelin, ETB | 0.025 nM 125I-Endothelin-1 | 0.1 μM Endothelin-1 | Human astrocytoma | >10,000a |
Estrogen | 0.1 nM 125I-3,7β-Estradiol | 10 nM 17β-Estadiol | Human breast cancer | >10,000a |
Galanin, nonselective | 0.07 nM 125I-Galanin | 100 nM Galanin (porcine) | Rat brain | >10,000a |
Glucocorticoid | 1 nM [3H]Dexamethasone | 10 μM Triamcinolone | Human recombinant | >10,000a |
Neurokinin, NK1 | 1.4 nM [3H]Substance P | 1 μM Substance P | Rat submaxillary gland | >10,000a |
Neurokinin, NK2 | 0.1 nM [125I-Neurokinin A | 1 μM Neurokinin A | Human recombinant CHO cells | 1510a |
Neurokinin, NK3 (NKB) | 0.1 nM 125I-Eledoisin | 1 μM Eledoisin | Rat cerebral cortex | >10,000a |
Oxytocin | 1 nM [3H]Oxytocin | 1 μM Oxytocin | Rat uterus | >10,000a |
Testosterone, cytosolic | 0.5 nM [3H]Methyltrienolone | 0.7 μM Methyltrienolone | Human LnCAP cells | >10,000a |
TRH | 2 nM [3H](3MeHis2)TRH | 10 μM TRH | Rat forebrain | >10,000a |
VIP, nonselective | 0.05 nM [125I]VIP | 1 μM VIP | Rat forebrain | >10,000a |
Vasopressin 1 | 0.5 nM [3H]Phenylalanyl-3,4,5-v | 1 μM Arg8-Vasopressin | Rat liver | >10,000a |
Ion channels: | ||||
Calcium, type L (benzothiazepine) | 5 nM [3H]cis-(+)-Diltiazem | 10 μM Diltiazem | Rat cerebral cortex | 751a |
Calcium, type L (dihydropyridine) | 0.2 nM [3H]Nitrendipine | 1 μM Nifedipine | Rat cerebral cortex | 1710a |
Calcium, type N | 0.01 nM 125I-ω-Conotoxin GVIA | 0.1 μM ω-Conotoxin GVIA | Rat cerebral cortex | >10,000a |
Chloride, GABA (t-butylbicycloorthobenzoate) | 20 nM [3H]t-Butylbicycloorthobenzoate | 10 μM t-Butylbicyclophosphorothionate | Rat cerebral cortex | >10,000a |
Potassium, ATP-sensitive | 0.2 nM [3H]Glibenclamide | 0.1 μM Glibenclamide | Rat cerebral cortex | >10,000a |
Potassium, Ca2+ act VI | 0.05 nM 125I-Apamin | 100 nM Apamin | Rat forebrain | >10,000a |
Potassium, human ether-a-go-go-related gene | 40 nM [3H]Astemizole | 100 μM Terfenadine | CHO cells | >10,000a |
Sodium, site 2 | 2 nM [3H]Batrachotoxin | 1 mM Aconitine | Rat forebrain | 1535a |
Enzymes and other miscellaneous | ||||
Acetylcholine esterase | 0.3 mM [3H]Acethylthiocholine | 100 μM Physostigmine | Human recombinant | >10,000a |
Choline acetyltransferase | 0.2 nM [14C]Acetyl coenzyme | 0.1 μM Ro 41-1049 | Rat cerebral cortex | >10,000a |
Glutamic acid decarboxylase | 4 μM [14C]l-Glutamic acid | 100 μM Aminooxy acetic acid | Rat striatum | >10,000a |
Leukotriene, LTB4 (BLT) | 0.48 nM [3H]Leukotriene B4 | 500 nM Leukotriene B4 | Guinea pig spleen | >10,000a |
Leukotriene, LTD4 (CysLT1) | 0.2 nM [3H]Leukotriene D4 | 1 μM Leukotriene D4 | Guinea pig lung | >10,000a |
MAOA oxidase, peripheral | 50 μM [14C]5-HT | 1 μM Ro 41-1049 | Rat liver mitochondria | >10,000a |
MAOB oxidase, peripheral | 10 μM [14C]Phenylethylamine | 10 μM Ro 16-6491 | Rat liver mitochondria | >10,000a |
Nitric-oxide synthase (NOS) | 5 nM [3H]l-NG-Nitro-arginine | 100 μM l-NG-Nitro-arginine | Rat brain | 1220a |
Platelet activating factor | 1.7 nM [3H]Hexadecyl-acetyl-platelet-activating factor | 1 μM C16-platelet-activating factor | Rabbit platelets | >10,000a |
Thromboxane, TXA2 | 2 nM [3H]SQ 29,548 | 10 μM Pinane-thromboxane | Human platelets | >10,000a |
CHO, Chinese hamster ovary; CRF, corticotrophin-releasing factor; TRH, thyrotropin releasing hormone; VIP, vasoactive intestinal peptide.
↵a These values were determined by NovaScreen. All other values were determined in-house using the assay conditions described under Materials and Methods.