In vitro pharmacology of RG3487: receptor binding, enzyme and cell-based assays
| Target | Control (10 μM) | Target | Control (10 μM) | Target | Control (10 μM) |
|---|---|---|---|---|---|
| % | % | % | |||
| A1 (h) | 97.5 | CCR1 (h) | 90.7 | Phospholipase A2 | 108 |
| A2A (h) | 94.5 | H1 (h) | 81.9 | COX1 (h) | 115 |
| A3 (h) | 95 | H2 (h) | 75.5 | COX2 (h) | 95.8 |
| a1 (nonselective) | 83 | MC4 (h) | 104 | 5-LO | 94.5 |
| α2 (non-selective) | 100 | ML1 (h) | 95.9 | Constituitive NOS (h) | 120 |
| β1 (h) | 77.3 | M1 (h) | 77.8 | Phosphodiesterase 1 | 99.8 |
| β2 (h) | 73 | M2 (h) | 87 | Phosphodiesterase 2 (h) | 99 |
| AT1 (h) | 76.3 | M3 (h) | 83.6 | Phosphodiesterase 3 (h) | 99.5 |
| AT2 (h) | 98.4 | M4 (h) | 90.4 | Phosphodiesterase 5 (h) | 108 |
| BZD (central) | 85.5 | M5 (h) | 101 | ACE (h) | 96.2 |
| BZD (peripheral) | 88.2 | P2X | 108 | ECE-1 (h) | 99.3 |
| BB (nonselective) | 103 | P2Y | 102 | Elastase (h) | 99.2 |
| B2 (h) | 91.9 | 5-HT1A (h) | 95.5 | Caspase-8 (h) | 107 |
| CGRP (h) | 101 | 5-HT1B | 88.3 | Cathepsin L (h) | 90.3 |
| CB1 (h) | 77.5 | 5-HT2A (h) | 51.4 | Neutral endopeptidase (h) | 88.3 |
| CCK1 (CCKA) (h) | 108 | 5-HT2C (h) | 73.1 | MMP-9 (h) | 96.4 |
| CCK2 (CCKB) (h) | 99.1 | 5-HT3 (h) | 0.1 | Tryptase (h) | 98.3 |
| D1 (h) | 94.3 | 5-HT5A (h) | 73.5 | Ca2+-ATPase pump | 107 |
| D2S (h) | 106 | 5-HT6 (h) | 77.6 | Phosphatase IB (h) | 99.2 |
| D3 (h) | 96.5 | 5-HT7 (h) | 84.7 | CAM kinase II | 105 |
| D4.4 (h) | 115 | σ (nonselective) | 70 | EGFR-tyrosine kinase (h) | 100 |
| D5 (h) | 86.2 | sst (nonselective) | 103 | ERK2 (P42mapk) | 99.3 |
| ETA (h) | 88.4 | VPAC1 (VIP1)(h) | 95.2 | PKA (h) | 109 |
| ETB (h) | 106 | V1a (h) | 86.3 | PKC | 98.8 |
| GABA (nonselective) | 74.8 | Ca2+ chan (L, verap site) | 82.7 | Acetylcholinesterase (h) | 101 |
| GAL1 (h) | 107 | K+ V chan | 89.8 | MAO-A (h) | 99.6 |
| GAL2 (h) | 82.5 | SK+ Ca chan | 94.5 | MAO-B (h) | 103 |
| PDGF | 104 | Na+ chan (site 2) | 52.7 | ATPase (Na+/K+) | 102 |
| CXCR2 (IL-8B) (h) | 109 | Cl− chan | 110 | AcetylCoA synthetase | 95.6 |
| TNF-α (h) | 94 | NE transporter (h) | 88.4 | Carbonic anhydrase II (h) | 88.3 |
h indicates human.