Table 2 Assessed couplings between G-proteins and serotonin receptors
From: How much do we know about the coupling of G-proteins to serotonin receptors?
Coupling G subunits | Not coupling G subunits | Notes | Second messengers | References |
|---|---|---|---|---|
5-HT1A receptor | ||||
Gαs-?-? | In guinea pig hippocampus | - | (Shenker, 1987) [[28]] | |
Gαi1-?-? | No(Gαs-?-?) | Human receptor and bovine G-proteins, in vitro reconstitution into E. coli membranes. Affinity order is Gαi3 > Gαi1 > Gαi2> > Gαo. | - | (Bertin, 1992) [[29]] |
Gαi2-?-? | ||||
Gαi3-?-? | ||||
Gαo-?-? | ||||
Gαi1-?-? | No(Gαs-?-?) | Human receptor transfected in human HeLa and hamster CHO cells; affinity order is Gαi3 > Gαi2 > Gαi1 | cAMP | (Raymond, 1993) [[30]] |
Gαi2-?-? | ||||
Gαi3-?-? | ||||
Gαi2-?-? | Human receptor transfected in hamster CHO cells | cAMP | (Gettys, 1994) [[31]] | |
Gαi3-?-? | ||||
Gαo-?-? | No(Gαs-?-?) | Human receptor transfected in insect Sf9 cells | - | (Mulheron, 1994) [[17]] |
No(Gαi1-?-?) | ||||
No(Gαi2-?-?) | ||||
No(Gαi3-?-?) | ||||
Gαi1-Gβ1-Gγ1 | Human receptor, rat Gαs, Gαi1, Gαi2, Gαi3, Gαo, murine Gαq, human Gαz, bovine Gβγ transfected in insect Sf9 cells. Gγ1 less effective than Gγ2, Gγ3, Gγ5, Gγ7. | - | (Butkerait, 1995) [[7]] | |
Gαi1-Gβ1-Gγ2 | ||||
Gαi1-Gβ1-Gγ3 | ||||
Gαi1-Gβ1-Gγ5 | ||||
Gαi1-Gβ1-Gγ7 | No(Gαs-Gβ1-Gγ2) | |||
Gαi2-Gβ1-Gγ2 | No(Gαq-Gβ1-Gγ2) | |||
Gαi3-Gβ1-Gγ2 | ||||
Gαo-Gβ1-Gγ2 | ||||
Gαz-Gβ1-Gγ2 | ||||
Gαq-Gβ1-Gγ2 | No(Gα12-Gβ1-Gγ2) | Human receptor, rat Gαs, murine Gαq, human Gαz, bovine Gβγ transfected in insect Sf9 cells; weak coupling with Gαq | - | (Barr, 1997) [[27]] |
Gαz-Gβ1-Gγ2 | No(Gα13-Gβ1-Gγ2) | |||
No(Gαs-Gβ1-Gγ2) | ||||
Gαi1-?-? | Human receptor and G-proteins transfected in hamster CHO cells, affinity order is Gαi2 > Gαi3, Gαi1, Gαo > Gαz | - | (Garnovskaya, 1997) [[32]] | |
Gαi2-?-? | ||||
Gαi3-?-? | ||||
Gαo-?-? | ||||
Gαz-?-? | ||||
Gαi1-?-? | Human receptor and rat Gαs transfected in insect Sf9 cells | - | (Clawges, 1997) [[14]] | |
Gαi2-?-? | ||||
Gαi3-?-? | ||||
Gαo-?-? | ||||
Gαz-Gβ1-Gγ2 | Human receptor and G-proteins transfected in Sf9 cells | - | (Barr, 1997) [[33]] | |
Gαi1-?-? | Rat receptor and G-proteins transfected in rat GH4C1 cells. | cAMP | (Liu, 1999) [[34]] | |
Gαi2-?-? | Human receptor and G-proteins transfected in human HeLa cells, affinity order is Gαi1 > Gαi2 > > Gαi3 | - | (Lin, 2002) [[35]] | |
Gαi3-?-? | ||||
Gαi2-?-? | No(Gαi1-?-?) | Rat receptor and G-proteins transfected in human HEK293 cells | cAMP | (Albert, 1999) [[36]] |
No(Gαi3-?-?) | ||||
No(Gαo-?-?) | ||||
Gαz-?-? | In rat hypothalamic paraventricular nucleus | - | (Serres, 2000) [[37]] | |
Gαi/o-?-? | Human receptor transfected in human HEK293 cells. | cAMP | (Malmberg, 2000) [[38]] | |
Gαs-?-? | ||||
Gαi3-?-? | Human receptor co-expressed with rat G-protein in monkey COS-7 cells. | - | (Dupuis, 2001) [[39]] | |
Human receptor transfected in hamster CHO cells. | - | (Newman-Tancredi, 2002) [[40]] | ||
Gαi1-?-? | No(Gαt-?-?) | Reconstitution in insect Sf9 cell expressing receptor and rat Gαi1 and bovine Gαt | - | (Slessareva, 2003) [[41]] |
Gαq-Gβ1-Gγ2 | Recombinant human receptor, mouse Gαq, rat Gαi2, bovine Gβγ co-expressed in insect Sf9. Strong coupling with Gαi2, weak with Gαq. | - | (Okada, 2004) [[42]] | |
Gαi2-Gβ1-Gγ2 | ||||
Gαi/o-?-? | No(Gαq-?-?) | In situ reconstitution in insect Sf9 cells with purified human receptor, squid Gαq, bovine Gαi and Gαo | - | (Okada, 2004) [[42]] |
No(Gαi1-?-?) | In rat cortex | - | (Mannoury la Cour, 2006) [[43]] | |
Gαo-?-? | No(Gαi2-?-?) | |||
Gαi3-?-? | No(Gαs-?-?) | |||
No(Gαz-?-?) | ||||
Gαi3-?-? | No(Gao-?-?) | In rat anterior raphe area | - | (Mannoury la Cour, 2006) [[43]] |
No(Gαi1-?-?) | ||||
No(Gαi2-?-?) | ||||
No(Gαs-?-?) | ||||
No(Gαz-?-?) | ||||
Gαo-?-? | No(Gαs-?-?) | In rat hippocampus | - | (Mannoury la Cour, 2006) [[43]] |
Gαi1-?-? | No(Gαz-?-?) | |||
Gαi3-?-? | No(Gαi2-?-?) | |||
Gαo-?-? | In rat hypothalamus | - | (Mannoury la Cour, 2006) [[43]] | |
Gαi1-?-? | No(Gαs-?-?) | |||
Gαi3-?-? | No(Gαi2-?-?) | |||
Gαz-?-? | ||||
Gαo-?-? | In rat hippocampus | - | (Martel, 2007) [[44]] | |
Gαi3-?-? | No(Gαi1-?-?) | |||
Gαs-?-? | ||||
Gαq-?-? | ||||
Gαi2-?-? | No(Gαs-?-?) | In rat dorsal raphe nucleus | cAMP | (Valdizán, 2010) [[45]] |
Gαi3-?-? | No(Gαz-?-?) | |||
Gαo-?-? | No(Gαi1-?-?) | |||
Gαi2-?-? | Human receptor transfected in hamster CHO cells | cAMP | (Rauly-Lestienne, 2011) [[46]] | |
Gαi3-?-? | ||||
5-HT1B receptor | ||||
Gαi1-?-? | Human receptor and rat Gα transfected in insect Sf9 cells | - | (Clawges, 1997) [[14]] | |
Gαi2-?-? | ||||
Gαi3-?-? | ||||
Gαo-?-? | ||||
Gαi1-?-? | No(Gαt-?-?) | Reconstitution in insect Sf9 cell expressing receptor and rat Gαi1 and bovine Gαt | - | |
- | ||||
- | ||||
Gαi2-?-? | Human receptor and rat G-proteins transfected in human HEK293 cells | cAMP | (Albert, 1999) [[36]] | |
Gαi-?-? | No(Gαs-?-?) | Chimpanzee receptor transfected in human HEK293 cells | - | (Alberts, 2000) [[49]] |
No(Gαq/11-?-?) | ||||
No(Gα13-?-?) | ||||
No(Gαo-?-?) | ||||
Gαi1-Gβ1-Gγ2 | Human receptor, rat Gα and bovine Gβγ proteins transfected in insect Sf9 cells | - | (Brys, 2000) [[50]] | |
Gαi1-?-? | Human receptor and G-proteins transfected in human HeLa cells, affinity order is Gαi1 > Gαi2 > > Gαi3 | - | (Lin, 2002) [[35]] | |
Gαi2-?-? | ||||
Gαi3-?-? | ||||
Gαi3-?-? | Human receptor transfected in hamster CHO cells | - | (Newman-Tancredi, 2003) [[51]] | |
5-HT1D receptor | ||||
Gαi3-?-? | Human receptor and rat Gα transfected in insect Sf9 cells | - | (Clawges, 1997) [[14]] | |
Gαi-?-? | No(Gαs-?-?) | Chimpanzee receptor transfected in human HEK293 cells | - | (Alberts, 2000) [[49]] |
No(Gαq/11-?-?) | ||||
No(Gα13-?-?) | ||||
No(Gαo-?-?) | ||||
Gαi1-Gβ1-Gγ2 | No(Gαq-Gβ1-Gγ2) | Human receptor, rat Gαi/o, mouse Gαq and bovine Gβγ proteins transfected in insect Sf9 cells | - | (Brys, 2000) [[50]] |
Gαi2-Gβ1-Gγ2 | ||||
Gαi3-Gβ1-Gγ2 | ||||
Gαo-Gβ1-Gγ2 | ||||
Gαi1-?-? | Human receptor and G-proteins transfected in human HeLa cells, affinity order is Gαi1 > Gαi2 > > Gαi3 | - | (Lin, 2002) [[35]] | |
Gαi2-?-? | ||||
Gαi3-?-? | ||||
5-HT1E receptor | ||||
No(Gαi3-?-?) | Human receptor and rat Gα transfected in insect Sf9 cells | - | (Clawges, 1997) [[14]] | |
5-HT1F receptor | ||||
Gαi-?-? | No(Gαs-?-?) | Monkey receptor transfected in human HEK293 cells | - | (Alberts, 2000) [[49]] |
No(Gαq/11-?-?) | ||||
No(Gα13-?-?) | ||||
No(Gαo-?-?) | ||||
5-HT2A receptor | ||||
Gαi/o-?-? | In mouse NIH3T3 cells | cPLA2 (not PLC, IP3) | (Kurrasch-Orbaugh, 2003) [[52]] | |
Gα12/13-?-? | ||||
Gαq-?-? | Rat receptor and G-protein transfected in human HEK293 cells. | Inositol Phosphate | (Bhatnagar, 2004) [[53]] | |
Human receptor and G-protein transfected in human HEK293 cells. | Inositol Phosphate | (Millan, 2012) [[54]] | ||
In rat cerebral cortical membranes. | - | (Odagaki, 2014) [[55]] | ||
Gα11-?-? | Human G-proteins transfected in rat cortex A1A1v cells | Inositol Phosphate | (Shi, 2007) [[56]] | |
Gαq-?-? | ||||
Gα11-?-? | Human G-proteins transfected in rat cortex A1A1v cells | Inositol Phosphate | (Shi, 2007) [[57]] | |
Gαq/11-?-? | Human receptor transfected in hamster CHO cells. | Ca2+ | (Cussac, 2008) [[58]] | |
In rat cortex. | - | (Mannoury La Cour, 2009) [[59]] | ||
5-HT2B receptor | ||||
Gαq/11-Gβ1-Gγ2 | Mouse receptors stably expressed in mouse fibroblast cells | Ras | (Launay, 1996) [[60]] | |
Gα13-?-? | No(Gαs-?-?) | In mouse LM6 and 1C11 and in M. natalensis carcinoid tumor primary cultured cells | IP3, NOS, cGMP | (Manivet, 2000) [[61]] |
No(Gαq/11-?-?) | ||||
No(Gαi-?-?) | ||||
Gαq/11-?-? | Human receptor transfected in hamster CHO cells | Ca2+ | (Cussac, 2008) [[58]] | |
Gαq-?-? | Human receptor and G-protein transfected in human HEK293 cells | Inositol Phosphate | (Millan, 2012) [[54]] | |
5-HT2C receptor | ||||
Gαi1-?-? | Mouse receptor and rat G-proteins expressed in Xenopus oocytes | - | (Chen, 1994) [[62]] | |
Gαo-?-? | ||||
Gαo-?-? | No(Gαs-?-?) | Mouse receptor and G-proteins expressed in Xenopus oocytes | Inositol Phosphate | (Quick, 1994) [[63]] |
Gαq-?-? | No(Gαolf-?-?) | |||
Gα11-?-? | No(Gαt-?-?) | |||
Gαq-?-? | No(Gαt-?-?) | Rat receptor and squid Gαq, bovine Gαt, Gαi/o proteins transfected in insect Sf9 cells | - | (Hartman, 1996) [[64]] |
No(Gαi/o-?-?) | ||||
Gαi-?-? | No(Gαs-?-?) | Human receptor in human HEK293 cells | IP3, cAMP | (Alberts, 1999) [[65]] |
No(Gαo-?-?) | ||||
No(Gαq/11-?-?) | ||||
No(Gα13-?-?) | ||||
Gαq-?-? | No(Gαs-?-?) | In rat choroid plexus epithelial cells | Inositol Phosphate | (Chang, 2000) [[66]] |
Gαq-?-?*# | No(Gα11-?-?)* | Human receptor and mouse G-proteins (except human Gα16) transfected in mouse NIH3T3 cells | Inositol Phosphate | (Price, 2001) [[67]] |
Gα11-?-?# | No(Gα12-?-?)*# | * with not edited receptor form | ||
Gα13-?-?* | No(Gα13-?-?)# | # with edited receptor form | ||
Gα15-?-?* | No(Gα14-?-?)*# | |||
No(Gα15-?-?)# | ||||
No(Gα16-?-?)*# | ||||
Gαi3-?-? | Human receptor transfected in hamster CHO cells | - | (Cussac, 2002) [[68]] | |
Gαq/11-?-? | ||||
Gαq-?-? | No(Gαs-?-?) | In rat choroid plexus epithelial cells and rat receptor transfected in mouse NIH3T3 cells | Inositol Phosphate (via PLD, not PLC) | (McGrew, 2002) [[69]] |
Gα13-?-? | ||||
Gαq-?-? | Human receptor and squid G-protein reconstitution in insect Sf9 cells. | Ca2+ | (Okada, 2004) [[70]] | |
Human receptor and G-protein transfected in human HEK293 cells. | Inositol Phosphate | (Millan, 2012) [[54]] | ||
Gαq-Gβ1-Gγ2 | Recombinant human receptor, mouse Gαq, rat Gαi2, bovine Gβγ co-expressed in insect Sf9. Strong coupling with Gαi2, weak with Gαq. | - | (Okada, 2004) [[42]] | |
Gαi2-Gβ1-Gγ2 | ||||
Gαq-?-? | No(Gαi/o-?-?) | In situ reconstitution in insect Sf9 cells with purified human receptor, squid Gαq, bovine Gαi and Gαo | - | (Okada, 2004) [[42]] |
Gαq/11-?-? | Human receptor transfected in hamster CHO cells | Ca2+ | (Cussac, 2008) [[58]] | |
5-HT4 receptor | ||||
Gαs-Gβ1-Gγ2 | No(Gαi2-Gβ1-Gγ2) | Murine receptor and G-proteins transfected in insect Sf9 cells | cAMP | (Ponimaskin, 2002) [[71]] |
No(Gαi3-Gβ1-Gγ2) | ||||
No(Gα12-Gβ1-Gγ2) | ||||
No(Gαq-Gβ1-Gγ2) | ||||
Gαs-?-? | Human receptor transfected in human HEK293 cells; 5HT4a receptor coupled only to Gαs, while 5HT4b isoform coupled to Gαs and Gαi/o | cAMP, Ca2+ | (Pindon, 2002) [[72]] | |
Gαi/o-?-? | (not IP3) | |||
Gαs-Gβ1-Gγ2 | No(Gαi2-Gβ1-Gγ2) | Murine receptor and G-proteins transfected in insect Sf9 cells | Inositol Phosphate, RhoA | (Ponimaskin, 2002) [[73]] |
Gα13-Gβ1-Gγ2 | No(Gα12-Gβ1-Gγ2) | |||
No(Gαq-Gβ1-Gγ2) | ||||
Gαs-?-? | Human receptor transfected in monkey COS-7 cells | cAMP, Inositol Phosphate | (Pellissier, 2011) [[74]] | |
5-HT5A receptor | ||||
No(Gαs-Gβ1-Gγ2) | Human receptor, rat Gαi/o, human Gαz and Gα16, bovine Gαs, mouse Gαq, Gα11, Gα12 and Gα13, bovine Gβγ reconstituted in insect Sf9 cells | - | (Francken, 2000) [[75]] | |
Gαi1-Gβ1-Gγ2 | No(Gαz-Gβ1-Gγ2) | |||
Gαi2-Gβ1-Gγ2 | No(Gαq-Gβ1-Gγ2) | |||
Gαi3-Gβ1-Gγ2 | No(Gα11-Gβ1-Gγ2) | |||
Gαo-Gβ1-Gγ2 | No(Gα12-Gβ1-Gγ2) | |||
No(Gα13-Gβ1-Gγ2) | ||||
No(Gα16-Gβ1-Gγ2) | ||||
Gαi1-Gβ1-Gγ2 | Human receptor, rat Gαi/o, human Gαz, bovine Gαs and Gβγ reconstituted in insect Sf9 cells | - | (Francken, 2001) [[76]] | |
Gαi2-Gβ1-Gγ2 | No(Gαs-Gβ1-Gγ2) | |||
Gαi3-Gβ1-Gγ2 | No(Gαz-Gβ1-Gγ2) | |||
Gαo-Gβ1-Gγ2 | ||||
Gαi/o-?-? | Human receptor transfected in rat C6 glioma cells | IP3, Ca2+, cAMP, cADPR | (Noda, 2003) [[77]] | |
5-HT6 receptor | ||||
Gαs-?-? | In human HEK293 cells stably expressing human receptor. | cAMP | (Baker, 1998) [[78]] | |
Human receptor and G-protein, assessed in vitro. | cAMP | (Kang, 2005) [[79]] | ||
5-HT7 receptor | ||||
Gαs-?-? | No(Gαi-?-?) | In human HEK293 cells stably expressing human receptor | cAMP, Ca2+/calmodulin | (Baker, 1998) [[78]] |
Gαs-?-? | No(Gαq/11-?-?) | Human receptor transfected in murine LM cells | cAMP | (Adham, 1998) [[80]] |
No(Gαi-?-?) | ||||
Gαs-?-? | No(Gαo-?-?) | Human receptor transfected in human HEK293 cells, affinity order is Gαs > Gαi = Gαq/11 | cAMP | (Alberts, 2001) [[81]] |
Gαi-?-? | No(Gα13-?-?) | |||
Gαq/11-?-? | ||||
Gαs-Gβ1-Gγ2 | No(Gαi2-Gβ1-Gγ2) | Murine receptor and G-proteins transfected in insect Sf9 cells | RhoA, Cdc42 (NOT Rac1) | (Kvachnina, 2005) [[82]] |
Gα12-Gβ1-Gγ2 | No(Gα13-Gβ1-Gγ2) | |||
No(Gαq-Gβ1-Gγ2) | ||||
Gαs-Gβ1-Gγ2 | No(Gαq-Gβ1-Gγ2) | Murine receptor and G-proteins transfected in insect Sf9 cells | cAMP | (Kvachnina, 2009) [[83]] |
Gα12-Gβ1-Gγ2 | No(Gαi-Gβ1-Gγ2) | |||
No(Gα13-Gβ1-Gγ2) |