Table 2.
Characterization of P1 receptors [Modified and updated from Burnstock (2003), with permission]
| P1 receptor | Agonists | Antagonists | Transduction mechanism | Patent utility |
|---|---|---|---|---|
| A1 | CCPA > R-PIA = S-ENBA | DPCPX | Gi/Go | Atrial fibrillation |
| N-0840 | cAMP ↓ | Cardioprotection | ||
| CVT-510 | MRS1754 | PLC ↑ | Diabetes, ischaemia | |
| GR79236 | WRC-0571 | |||
| A2A | HENECA > CGS21680 = CVT-3146 | KF17837 | GS | Inflammation |
| SCH 58261 | cAMP ↑ | Asthma | ||
| ZM241385 | IP3 ↑ | COPD | ||
| ATL-146e | KW 6002 | Parkinson's disease | ||
| A2B | Bay60-6583 | PBS603 | GS | Bowel and bladder abnormalities |
| MRE-2029-F20 | cAMP ↑ | |||
| PSB0788 | PLC ↑ | |||
| MRS 1706 | ||||
| PSB 1115 | ||||
| Alloxazine | ||||
| A3 | IB-MECA > 2-Cl-IB-MECA | MRS1220 | Gi/Go | Cardioprotection, cerebrovascular ischaemia, cancer, allergy |
| L-268605 | Gq/G11 | |||
| DBXRM | MRS 1191 and 1334 (h) | cAMP ↓ | ||
| VT160 | MRS 1523 (r) | IP3/DAG ↑ | ||
| HEMADO | VUF 8504 and 5574 | PLC ↑ | ||
| PSB10 |
CCPA, 2-chloro-N6-cyclopentyladenosine; COPD, chronic obstructive pulmonary disease; DBXRM, xanthine 7-riboside derivative; DPCPX, 8-cyclopentyl-1,3-dipropulxanthine; HEMADO, 2-(1-hexynyl)-N-methyladenosine; HENECA, 2-hexynyl-5′-N-ethylcarboxamidoadenosine; IB-MECA, N6-(3-iodobenzyl) adenosine-5′-N-methylcarboxamide; 2CI-1B-MECA, 2-chloro-N6-(3-iodobenzyl) adenosine-5′-N-methyluronamide; R-PIA, N6-phenylisopropyladenosine; S-ENBA, (2S)-N6-(2-endo-norbornyl) adenosine.