Pharmacological profile for CL receptor/RAMP complexes
| Receptor | αCGRP | βCGRP | CGRP8–37 | AM | AM22–52 | AMY | Cell | References |
|---|---|---|---|---|---|---|---|---|
| hCL receptor/hRAMP1 | 10 | 11 | 9.5 | 8.1 | 6.4 | NS | Swiss3T3 | McLatchie et al., 1998 |
| 10.3 | 9 | 7.8 | HEK293 | Aiyar et al., 1996 | ||||
| 9.6 | 9.8 | 9.1 | 6.8 | HEK293 | Aiyar et al., 2001 | |||
| rCL receptor/rRAMP1 | 8.9 | 9.3 | 8.2 | 8.8 | >6 | 7.8 | UMR106 | Oliver et al., 2001 |
| rCL receptor/hRAMP1 | 8.3 | 8.4 | 8.9 | >7 | >6 | >6 | COS-7 | Buhlmann et al., 1999 |
| 7.9 | 8.3 | 8.8 | 6.9 | >6 | >6 | UMR106 | Buhlmann et al., 1999 | |
| 8.2 | 8.3 | 8.8 | 6.9 | Schneider | Aldecoa et al., 2000 | |||
| rCL receptor/mRAMP1 | 8.4 | 8.2 | 8.8 | 6.8 | COS-7 | Husmann et al., 2000 | ||
| pCL receptor/hRAMP1 | 10 | 9.8 | 9.18 | 7.7 | HEK293 | Elshourbagy et al., 1998 | ||
| 9.5 | 10.2 | 9.1 | 8.2 | HEK293 | Aiyar et al., 2001 | |||
| hCL receptor/hRAMP2 | 5.9 | 6.5 | 7.1 | 9.2 | 7.8 | NS | Swiss3T3 | McLatchie et al., 1998 |
| 6.3 | 6.8 | 7.2 | 9.1 | 7.7 | NS | HEK293 | Fraser et al., 1999 | |
| 7.7 | >5 | 8.5 | 7.0 | HEK293 | Aiyar et al., 2001 | |||
| rCL receptor/rRAMP2 | >7 | >7 | >6 | 9.3 | 7 | >6 | UMR106 | Oliver et al., 2001 |
| rCL receptor/hRAMP2 | >6 | 7.1 | 8.8 | 8.5 | >6 | COS-7 | Buhlmann et al., 1999 | |
| >6 | 7.0 | 7.4 | 9.5 | 8.6 | >6 | UMR106 | Buhlmann et al., 1999 | |
| 6.7 | 6.7 | 7.0 | 9.1 | 7.9 | Schneider | Aldecoa et al., 2000 | ||
| rCL receptor/mRAMP2 | 6.8 | 7.0 | 8.7 | 8.5 | COS-7 | Husmann et al., 2000 | ||
| pCL receptor/hRAMP22-150 | 8.6/7.5 | 8.8/7.2 | 7.7/6.2 | 9.0/8.6 | 7.14 | HEK293 | Aiyar et al., 2001 | |
| hCL receptor/hRAMP3 | 6.5 | 7.1 | 7.3 | 8.3 | 7.1 | HEK293 | Fraser et al., 1999 | |
| 6.8 | 7.3 | 7.3 | 8.9 | 7.3 | HEK293 | Aiyar et al., 2001 | ||
| rCL receptor/mRAMP3 | 7.7 | 7.7 | 8.4 | 8.2 | 7.8 | COS-7 | Husmann et al., 2000 | |
| pCL receptor/hRAMP32-150 | 8.3/7.0 | 9.2/7.5 | 8.2/>5 | 9.4/9.2 | 7.2 | HEK293 | Aiyar et al., 2001 |
r, rat; m, mouse; p, pig. Values represent pIC50values measured against 125I-CGRP (normal text) or125I-adrenomedullin (italics). Displacing ligands are of human for hCL receptor and pCL receptor; otherwise rat. Schneider cells are from Drosophila.
↵2-150 hαCGRP showed low potency in stimulating cAMP production in the presence of RAMP2 or RAMP3 (pEC50 values of 6.8 and 6.5) in spite of high affinity binding.