Table 1.
Effects of major GPCRs on lipolysis.
| GPCR | IUPHAR Name | Coupling | Molecular Targets a | Lipolysis b |
|---|---|---|---|---|
| beta 1 adrenergic | β1-adrenoceptor | Gs > Gi | AC, PKA, GC | + |
| beta 2 adrenergic | β2-adrenoceptor | Gs > Gi | AC, PKA, GC | + |
| beta 3 adrenergic | β3-adrenoceptor | Gs > Gi | AC, PKA, HSL, GC | + |
| A1R | A1 receptor | Gi > Gs, Gq | AC, PLC | − |
| A2AR | A2A receptor | Gs > Gq | AC, PLC | + |
| A2BR | A2B receptor | Gs > Gq | AC, PLC | + |
| D1 | D1 receptor | Gs | AC, PLC | − |
| D2 | D2 receptor | Gi | AC | − (+humans) |
| 5-HT2A | 5-HT2A receptor | Gq > Gi | PLC, AC | − |
| FFAR4/GPR120 | FFA4 receptor | Gq | PLC | + (?) |
| FFAR1/GPR40 | FFA1 receptor | Gq > Gs | AC, PLC, PLA2 | + |
| CB1 | CB1 receptor | Gi > Gs | AC | − |
| GPER | GPER | Gi > Gs | PLC, AC | + |
| GprC6A | GPRC6 receptor | Gq | PLC | + (?) |
| GPR183/EBI2 | GPR183 | Gi | AC | − |
| ETA | ETA receptor | Gq | PLC, PLA2, PLD | + |
| CMKLR1 | Chemerin receptor 1 | Gi | AC | +/− |
| Apelin | Apelin receptor | Gi | AC, PKC | − |
| NPY1 | Y1 receptor | Gi | AC | − |
| GPR74 | NPPF2 | Gi (?) | AC | − |
| Gpr64 | ADGRG2 | Gs > Gq | AC, PLC | + |
| Gpr3 | GPR3 | Gs | AC | + |
| Olfr544 | none | Golf/Gs | ? | + |
| Opn3 | OPN3 | Gs (?) | ? | + |
a most known molecular targets; if unknown, not specific for adipocytes. Note: β-arrestins coupling was not indicated. b + stimulatory effects, − inhibitory effects. ? not well defined. AC: Adenylate cyclase; PKA: protein kinase A; GC: guanylate cyclase; HSL: hormone sensitive lipase; PLC: phospholipase C; PLA2: phospholipase A2; PLD, phospholipase D; PKC: protein kinase C.