Effect of 10 μM AMG8562 on the specific radioligand binding to the receptors, ion channels, or enzymes studied
Ki values are shown in parentheses for compounds that showed greater than 50% inhibition at 10 μM.
Target | Ligand | % Inhibition of Specific Binding (Ki) |
|---|---|---|
| A2A (h) | [3H]CGS 21680 | -16 |
| α1 (nonselective) | [3H]Prazosin | 1 |
| α2 (nonselective) | [3H]RX 821002 | -2 |
| β1 (h) | [3H](-)-CGP 12177 | 20 |
| AT2 (h) | [125I]CGP 42112A | -3 |
| B1 (h) | [3H]desArg10-KD | 9 |
| B2 (h) | [3H]Bradykinin | -2 |
| CGRP (h) | [125I]hCGRPα | 2 |
| CB1 (h) | [3H]CP 55940 | 53 (9.5 μM) |
| CB2 (h) | [3H]WIN 55212-2 | 26 |
| CCKA (h) (CCK1) | [125I]CCK-8 | 70 (16 μM) |
| D1 (h) | [3H]SCH 23390 | 22 |
| D2S (h) (agonist site) | [3H]7-OH-DPAT | 15 |
| D3 (h) (agonist site) | [3H]7-OH-DPAT | 10 |
| ETA (h) | [125I]Endothelin-1 | 6 |
| GABA (nonselective) | [3H]GABA | -3 |
| GAL2 (h) | [125I]Galanin | 10 |
| CXCR2 (h) (IL-8B) | [125I]Interleukin-8 | 17 |
| CCR1 (h) | [125I]MIP-1α | -13 |
| Ghrelin (h) (GHS) | [125I][His]-ghrelin | -13 |
| H1 (h) | [3H]Pyrilamine | -3 |
| H2 (h) | [125I]APT | 9 |
| H3 (h) | [3H]Nα-Me-histamine | 15 |
| H4 (h) | [3H]Histamine | 1 |
| LTB4 (h) (BLT1) | [3H]LTB4 | 14 |
| LTD4 (h) (CysLT1) | [3H]LTD4 | 8 |
| Edg-2 (LPA) (h) | [3H]LPA | 15 |
| MC4 (h) | [125I]NDP-α-MSH | 17 |
| MT1 (h) | [125I]Iodomelatonin | 81 (2.9 μM) |
| M1 (h) | [3H]Pirenzepine | 33 |
| M3 (h) | [3H]4-DAMP | 9 |
| NK1 (h) | [125I]BH-SP | 25 |
| N (neuronal) (α-BGTX-insensitive) (α4β2) | [3H]Cytisine | -4 |
| κ-Opioid (KOP) | [3H]U 69593 | 53 (14 μM) |
| μ-Opioid (h) (MOP) (agonist site) | [3H][d-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin | 15 |
| PAF (h) | [3H]C16-PAF | 4 |
| PCP | [3H]TCP | 18 |
| TXA2/PGH2 (h) (TP) | [3H]SQ 29548 | 40 |
| P2X | [3H]α,β-methylene-ATP | 8 |
| P2Y | [35S]dATPαS | 0 |
| 5-HT1A (h) | [3H]8-OH-DPAT | 8 |
| 5-HT2B (h) (agonist site) | [125I](±)-DOI | 82 (8.9 μM) |
| 5-HT3 (h) | [3H]BRL 43694 | 2 |
| Sst (nonselective) | [125I]Tyr11-somatostatin-14 | 12 |
| VIP1 (h) (VPAC1) | [125I]VIP | -1 |
| VIP2 (h) (VPAC2) | [125I]VIP | 5 |
| V1a (h) | [3H]AVP | 5 |
| Ca2+ channel (L, DHP site) | [3H](+)-PN 200-110 | 69 (1.7 μM) |
| Ca2+ channel (N) | [125I]ω-Conotoxin GVIA | -3 |
| Na+ channel (site 2) | [3H]Batrachotoxinin | 52 (3.2 μM) |
CCK, cholecystokinin; VIP, vasoactive intestinal peptide; AVP, arginine vasopressin; LPA, lysophosphatidic acid; DOI, (±)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane; BRL 43694, granisetron; SQ 29548, [1S-[1a,2a(Z),3a,4a]]-7-[3-[[2-[(phenylamino)carbonyl]hydrazino]methyl]-7-oxabicyclo[2.2.1]-hept-2-yl]-5-heptanoic acid; 4-DAMP, 4-diphenylacetoxy-N-[2-chloroethyl]piperidine hydrochloride; CGP 42112A, N-α-nicotinoyl-Tyr-(N-α-CBZ-Arg)-Lys-His-Pro-Ile-OH; 7-OH-DPAT, 7-hydroxy-2-dipropylaminotetralin; LTB4, leukotriene B4; LTD4, leukotriene D4; NDP-α-MSH, [Nle4-d-Phe7]α-melanocyte-stimulating hormone; APT, aminopotentidine; MIP, macrophage inflammatory protein; C16-PAF, 1-O-hexadecyl-2-O-acetyl-sn-glycero-3-phosphocholine; TCP, N-[1-(2-thienyl)cyclohexyl]piperidine; CGRP, calcitonin gene-related peptide; DHP, dihydropyridine; desArg 10-KD, desArg 10-kallidin; BH-SP, Bolton Hunter substance P; TXA1/PGH2, thromboxane A2/prostaglandin endoperoxide H2; P2X, purinergic receptor 2X; P2Y, purinergic receptor 2Y; h, human.