Table 2.
Panel of receptors and ion channels used to evaluate CRH1antagonist selectivity
| Class | Receptor/ion channel/transporter |
|---|---|
| Adenosine | A1, A2A, A3 |
| Adrenergic | α 1, α 2, β 1, β 2, NET |
| Angiotensin | AT1, AT2 |
| Benzodiazepine | Central, peripheral |
| Bombesin | BB (nonselective) |
| Bradykinin | B2 |
| CGRP | CGRP1 |
| Canabinoid | CB1 |
| Cholecystokinin | CCK1, CCK2 |
| Dopamine | D1, D2S, D3, D4.4, D5, DAT |
| Endothelin | ETA, ETB |
| GABA | Nonselective |
| Galanin | GAL1, GAL2 |
| PDGF | PDGF |
| IL-8 | CXCR2 |
| TNF-α | TNF-α |
| CCR1 | CCR1 |
| Histamine | H1, H2 |
| Melanocortin | MC4 |
| Muscarinic | M1, M2, M3 |
| Tachykinin | NK1, NK2, NK3 |
| Neuropeptide Y | Y1, Y2 |
| Neurotensin | NT1 |
| Opioid | MOP, DOP, KOP, NOP |
| PACAP | PAC1 |
| PCP | PCP |
| TXA2/PGH2 | TXA2/PGH2 |
| Purine | P2X, P2Y |
| Serotonin | 5-HT1a, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6, 5-HT7 |
| σ | Nonselective |
| Somatostatin | Nonselective |
| VIP | VIP1 |
| Vasopressin | V1a |
| Ca2+ channel | L type |
| K+ channel | K+ V channel |
| SK+ Ca channel | SK+ Ca channel |
| Na+ channel | Site 2 |
| Cl− channel | Cl− channel |
At a 10 μm concentration, MTIP did not induce a 50% inhibition at any of the targets listed.