Pharmacological selectivity of A-425619
Target | Ligand | ∼IC50 |
|---|---|---|
| μM | ||
| Adenosine A1 | [3H]DPCPX | >10 |
| Adenosine A2A | [3H]CGS 21680 | >10 |
| Adenosine A3 | [125I]I-AB-MECA | >10 |
| Adrenergic α1 | [3H]Prazosin | >10 |
| Adrenergic α2 | [3H]RX821002 | >10 |
| Adrenergic β1 | [3H](–)CGP 12177 | >10 |
| Adrenergic β2 | [3H](–)CGP 12177 | >10 |
| ANP | [125I]ANP | >10 |
| Cannabinoid CB1 | [3H]Win 55212-2 | >10 |
| Cannabinoid CB2 | [3H]Win 55212-2 | >10 |
| Dopamine D1 | [3H]SCH 23390 | >10 |
| Dopamine D2 | [3H]Spiperone | >10 |
| Dopamine D3 | [3H]Spiperone | >10 |
| Dopamine D4.4 | [3H]Spiperone | >10 |
| Dopamine D5 | [3H]SCH 23390 | >10 |
| GABA | [3H]GABA | >10 |
| IL-8B (CXCR2) | [125I]IL-8 | >10 |
| TNFα | [125I]TNFα | >10 |
| CCR1 | [125I]MIP-1α | >10 |
| Histamine H1 | [3H]Pyrilamine | >10 |
| Histamine H2 | [125I]APT | >10 |
| Muscarinic M1 | [3H]Pirenzepine | >10 |
| Muscarinic M2 | [3H]AF-DX384 | >10 |
| Muscarinic M3 | [3H]4-DAMP | >10 |
| Muscarinic M4 | [3H]4-DAMP | >10 |
| Muscarinic M5 | [3H]4-DAMP | >10 |
| Opioid δ2 | [3H]DADLE | >10 |
| Opioid κ | [3H]U 69593 | >10 |
| Opioid μ | [3H]DAMGO | >10 |
| ORL1 | [3H]Nociceptin | >10 |
| PACAP PAC1 | [3H]PACAP1–27 | >10 |
| P2X | [3H]α,βMeATP | >10 |
| P2Y | [35S]dATPαS | >10 |
| Serotonin 5-HT1A | [3H]8-OH-DPAT | >10 |
| Serotonin 5-HT1B | [3H]CYP | >10 |
| Serotonin 5-HT2A | [3H]Ketanserin | >10 |
| Serotonin 5-HT2C | [3H]Mesulergine | >10 |
| Serotonin 5-HT3 | [3H]BRL 43694 | >10 |
| Serotonin 5-HT5A | [3H]LSD | >10 |
| Serotonin 5-HT6 | [3H]LSD | >10 |
| Serotonin 5-HT7 | [3H]LSD | >10 |
| σ1 | [3H]Pentazocine | >10 |
| Angiotensin AT1 | [125I][Sar1,Ile8]-ATII | >10 |
| Angiotensin AT2 | [125I]CGP 42112A | >10 |
| Bombesin | [125I][Tyr4]bombesin | >10 |
| Bradykinin B2 | [3H]NPC 17731 | >10 |
| CCKA | [3H]Devazepide | >10 |
| CCKB | [3H]CCK-8 | >10 |
| Endothelin ETA | [125I]Endothelin-1 | >10 |
| Endothelin ETB | [125I]Endothelin-1 | >10 |
| Galanin GAL1 | [125I]Galanin | >10 |
| PDGF | [125I]PDGF BB | >10 |
| Melatonin ML1 | [125I]Iodomelatonin | >10 |
| Neurokinin NK1 | [125I][Sar9,Met(O2)11]-S | >10 |
| Neurokinin NK2 | [125I]NKA | >10 |
| Neurokinin NK3 | [125I][MePhe7]-NKB | >10 |
| Neuropeptide Y1 | [125I]Peptide YY | >10 |
| Neuropeptide Y2 | [125I]Peptide YY | >10 |
| Neurotensin NT1 | [125I]Neurotensin | >10 |
| Somatostatin | [125I]Tyr11-somatostatin | >10 |
| VIP1 (VPAC1) | [125I]VIP | >10 |
| Vasopressin V1a | [3H]AVP | >10 |
| Norepinephrine transporter | [3H]Nisoxetine | >10 |
| Dopamine uptake | [3H]GBR 12935 | >10 |
| Benzodiazepine Central | [3H]Flunitrazepam | >10 |
| Benzodiazepine Peripheral | [3H]PK 11195 | 5 |
| AMPA | [3H]AMPA | >10 |
| Kainate | [3H]Kainic acid | >10 |
| NMDA | [3H]CGP 39653 | >10 |
| Ca2+ channel DHP site | [3H]PN200-110 | >10 |
| Ca2+ channel diltiazem site | [3H]Diltiazem | >10 |
| Ca2+ channel verapamil site | [3H]D 888 | >10 |
| Ca2+ channel N | [125I]ω-Conotoxin | >10 |
| K+ channel (volt. Dependent) | [125I]Dendrotoxin | >10 |
| K+ channel (Ca2+ dependent) | [125I]Apmin | >10 |
| Na+ channel (Site 2) | [3H]Batrachotoxinin | >10 |
| Cl- ionophore | [35S]TBPS | >10 |
| Glycine (strychnine-sensitive) | [3H]Strychnine | >10 |
| Glycine (strychnine-insensitive) | [3H]MDL105,519 | >10 |
| MAO-A | [3H]Ro41-1049 | >10 |
| MAO-B | [3H]Ro-19-6327 | >10 |
| σ | [3H]DTG | 10 |
| σ2 | [3H]DTG | >10 |
DPCPX, 8-cyclopentyl-1,3-dipropylxanthine; AB-MECA, 4-aminobenzyl-5′-N-methylcarboxamidoadenosine; ANP, atrial natriuretic peptide; IL, interleukin; TNF, tumor necrosis factor; MIP, macrophage inflammatory protein; APT, aminopotentidine; 4-DAMP, 4-diphenylacetoxy-N-methylpiperidine; DAMGO, [d-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin; α,βMeATP, α,β-methyleneadenosine 5′-triphosphate; [35S]dATPαS, 2′deoxyadenosine-5′-[α-35S]-thiotriphosphate; 8-OH-DPAT, 8-hydroxy-2-dipropylaminotetralin; LSD, lysergic acid diethylamide; PDGF, platelet-derived growth factor; NKA, neurokinin A; VIP, vasoactive intestinal peptide; AVP, arginine vasopressin; AMPA, α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid; NMDA, N-methyl-d-aspartate; DHP, dihydropyridine; TBPS, t-butylbicyclophosphorothionate; MAO, monoamine oxidase; DTG, 1,3-di(2-tolyl)guanidine.