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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 - (Bae, 1997; Bae, 1999; Slessareva, 2003) [[41],[47],[48]]
-
-
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)
  1. “?” means that the particular Gβ or Gγ protein has not be identified in the reference paper. “-” means that the second messenger has not be assessed in the reference paper. Note: unfortunately some papers reported Gαi/o, Gαi, or Gαq/11 without further distinction. Abbreviations: RhoA: Ras homolog gene family, member A; Cdc42: cell division control protein 42; Rac1: Ras-related C3 botulinum toxin substrate 1; cADPR: cyclic adenosine diphosphoribose; PLD: phospholipase D; NOS: nitric-oxide synthase; cGMP: cyclic guanosine monophosphate; cPLA2: cytosolic phospholipases A2.