Table 2.
GPCR expressed in heart: Gα coupling and pharmacological way to modulate their signaling.
| Receptor | Subtype | Coupling | Example of agonist | Antagonist |
|---|---|---|---|---|
| α-Adrenergic | la, lb, 1D, | Gq | Phenylephrine, Methoxamine | Corynanthiane, Prazosin |
| 2a, 2c | Gi | UK14304, B-HT92O | Yohimbine, RX821002 | |
| β-adrenergic | β1, β2, β3 | Gs, Gi | Isoproterenol | Alprenolol, Pindolol, Propranolol |
| Adenosine | Adoral, | Gi | CHA, CPA | CPX, CPT, N-0840 |
| 2a,2b | Gs | CGS21680, DPMA, HENECA | KW6002, Alloxazine, SCH-58261 | |
| Adrenomodulin | CGRP | Gi, Gs | ||
| Angiotensin | AT1a | Gq, Gi | AngII, AngIII L162313 | Losartan, Candesartan |
| AT2 | Gi | AngII, AngIII CGP42112A | PD123319, L-159686 | |
| Apelin | APJ | Gi | Apelin13 | |
| AVPR1a | Gq | vasopressin | Relcovaptan | |
| Bradykinin | Bdkrbl, 2 | Gq | Lys-BK | B9430 |
| Calcium sensing | Ca-SR | Gs | ||
| Cannabinoid | CB1 | Gi | THC, CP-5594O, Nabilone | SR141716A, AM25l |
| Chemokine receptor | CX3CR1, | Gi | Fractalkine | |
| CXCR2 | Cri | IL-8, GCP2 | ||
| CXCR4,7 | Gi | SDF1α | AMD3100 | |
| CXCR6 | Gi | CXCL16 | ||
| CCBP2, | Gi | |||
| CCR1, 5 | Gi | MIP1α | ||
| CCR2 | Gi | MCP-1 | ||
| CCR10 | Gi | CTACK | ||
| XCR1 | Gi | xCL1 | ||
| Complement component receptor | C3aRl, C5R1 | Gi | ||
| Corticotropin releasing hormone | CRHR2 | Gs | CRF, UCN1 | Astressin |
| Cysteinyl leukotriene | Cystl1 | Gq | LTD4 | Cinalukast |
| Dopamine | Drd2 | Gi | U-91356A, TNPA | L-741626 |
| Drd3 | Gi | PD128907, BP897 | Nafadotride, GR103691 | |
| Endothelin | ET-A, ET-B | Gq | ET1 | PD142893 |
| Frizzled | Fzdl, 2, 3, 5, 6, 7, 8 | |||
| Galanin | GalR2 | Gq | Galanin, GALP | Galantide |
| GLP1 | Gs | |||
| Glucagon | Gq, Gs | |||
| Gonadotropin receptor | LGR6, 7 | Gi, Gq | ||
| GPCR5 | Raig2, GPCR5c | ? | ||
| Growth hormone secretagogue-receptor | GHS-R1a | GS, Gq | ||
| Histamine | H1 | Gq | Pyrilamine | |
| H2 | Gs | Amthamine | Cimetidine | |
| H3 | Gi | Immethridine | Ciproxifan | |
| Latrophilin | Lphn1, 2 | 011-15 | alpha-Latrotoxin | |
| Mas | Mas1, GPR168 | ? | ||
| Melanin concentrating hormone | SLC-1 | ? | MCH | SNAP794l |
| Melanocortin | MC3R | Gs | γ2-MSH | SHU9119 |
| Melatonin | MT1 | Gi, Gq | Melatonin, S20098 | Luzindole |
| MT2 | Gi | Melatonin, S20098 | Luzindole | |
| Muscarinic | M2, M3 | Gi, Gq | Bethanecol, Xanomeline, Metoclopramine | Gallamine, Atropine, Scopolamine |
| Neuromedin U | NMUl, NMU2 | Gi, Gq | NMU | |
| Neuropeptide Y receptor | NPY1, 2 | Gi | NPY | BIBP3226, BIIE0246 |
| Nucleotide | P2Y1 | Gq | 2MeSADP | BzATP, Suramin |
| P2Y2 | Gq, Gi | UTPγs | Suramin | |
| P2Y4 | Gq, Gi | UTP | ATP | |
| P2Y5 | Gi, G12/13 | |||
| P2Y6 | Gq | UDP | Suramin | |
| P2Y11 | Gq, Gs | BzATP | Suramin | |
| P2Y13 | Gi | 2MeSADP | Ap4A | |
| P2Y14 | Gi | UDP-glucose | ||
| Opioid | MOP | Gi | DAMGO | Cyprodime |
| DOP | Gi | DPDPE | Naltrindole | |
| KOP | Gi | Enadoline | GNTI | |
| Opsin | Opn4 | Gi, Gq | ||
| Oxytocin | OXTR | Gq | Oxytocin, Carbetocin | |
| P518RF amide | SP9155 | ? | P518 | |
| Vasoactive Intestinal Peptide receptor | VIPR2 | Gs, Gq | VIP | acetyl-His-PheLysArg-VIP-GRF |
| PAR | PAR1 | Gi, Gq, G12/13 | Thrombin, Trypsin | BMS200261 |
| PAR2 | Gi, Gq | Trypsin | ||
| PAR4 | Gq | Thrombin, Trypsin | t-cinnamoylYPGKF | |
| Platelet-activating factor receptor | PTAFR | Gq | PAF | Israpafant |
| Prolactin releasing peptide | GR3 | |||
| Prostacyclin | Ptgir | Gs | ||
| Prostanoid | EP1 | Gq | Iloprost | SH-19220 |
| EP4 | Gs | ONO-AE1-734 | AH23848 | |
| Relaxin-H2 | LGR7, Rxfp4 | Gi | ||
| Serotonin | 5HTR1a | Gi | R(+)-8-OH-DPAT | Spiperone |
| 5HTR1b | Gi | Sumatriptan, CGS12066 | GR55562, SB216641 | |
| 5HTR2b | Gq | BW723C86 | YM348 | |
| 5HT4 | Gs | BIMU8 | GR113808 | |
| Smoothened | Smoh | Gi | ||
| Somatostain | SSTR3 | Gi | L-796778 | NVP-ACQ090 |
| SSTR4 | Gi | NNC26-9100 | s | |
| Sphingosine | Edg1 | Gi | S1P, FTY720-P | VPC23019 |
| Edg5 | Gq,Gi G12/13 | S1P | JTE-013 | |
| Edg3 | Gq, Gi, G12/13 | S1P, FTY720-P | VPC23019 | |
| LPA | Edg2 | Gi, G12 13 | 1-oleyl-LPA | VPC32183 |
| Substance P | NK-1 | Gq | substance P | GR-82334 |
| Thromboxan | Tbxa2r | Gq | Thromboxan | Seratrodast |
| Urotensin | GPR14 | Gq | UII | [Cha6]U-II(4-11) |
| Other GPCR expressed in Heart | ||||
| CD97 | GPR77(C5L2) | |||
| ELTD1 | GPR82 | |||
| EMR1 | GPR107 | |||
| TM7SF3 | GPR108 | |||
| GPR1 | GPR116 | |||
| GPR10 | GPR120 | |||
| GPR17 | GPR124 | |||
| GPR2l | GPR125 | |||
| GPR22 | GPR133 | |||
| GPR27 | GPR135 | |||
| GPR30 | GPR137 | |||
| GPR31 | GPR137b | |||
| GPR34 | GPR146 | |||
| GPR4 | GPR153 | |||
| GPR44 | GPR161 | |||
| GPR48 | GPR175 | |||
| GPR54 | GPR182 | |||
| GPR56 | GPR183 (Ebi2) | |||
This table summarized the list of mRNA encoding for GPCRs detected in the whole cardiac tissue (cardiomyocytes, endothelial cells, fibroblasts…) extracted from (Hakak et al., 2003; Katugampola and Davenport, 2003; Tang and Insel, 2004; Regard et al., 2008; Moore-Morris et al., 2009), the main known Gα protein coupling, an example of an agonist and an antagonist (this list is non-exhaustive and selectivity for each molecule is not discussed).