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Table 1.
Summary of GPCR agonists and cAMP analogs analyzed using the pRII assay in rat or mouse sensory neurons
CompoundActionLipophilicity (log K′g)aEC50 or IC50 for ratbEC50 or IC50 for mousebReference
5-HT Gs-GPCR agonist  14 nM 47 nM Isensee et al., 2014a, 2017a  
Prostaglandin I2 Gs-GPCR agonist  74 nM 27 nM Isensee et al., 2014a, 2017a  
Prostaglandin D2  Gs-GPCR agonist  377 nM  Isensee et al., 2014b  
DAMGOc Gi-GPCR agonist  321 nM  Isensee et al., 2017a  
Fentanyl Gi-GPCR agonist  97 nM 36 nM Isensee et al., 2017a  
Fsk Activator  1.7 µM 2.6 µM Isensee et al., 2014a, 2017a  
Sp-8-Br-cAMPS Activator 1.66 203 µM  This study 
Sp-8-Br-cAMPS-AM Activator  1.3 µM 6.8 µM Isensee et al., 2014a, 2017a  
Rp-cAMPS Inhibitor 1.21   Schwede et al., 2015  
Rp-cAMPS-pAB Inhibitor  ∼10 µM  This study 
Rp-8-pCPT-cAMPS Inhibitor 2.72   This study 
Rp-8-pCPT-cAMPS-pAB Inhibitor  ∼4 µM  This study 
Rp-8-Br-cAMPS Inhibitor 1.47   This study 
Rp-8-Br-cAMPS-pAB Inhibitor  ∼3 µM  This study 
CompoundActionLipophilicity (log K′g)aEC50 or IC50 for ratbEC50 or IC50 for mousebReference
5-HT Gs-GPCR agonist  14 nM 47 nM Isensee et al., 2014a, 2017a  
Prostaglandin I2 Gs-GPCR agonist  74 nM 27 nM Isensee et al., 2014a, 2017a  
Prostaglandin D2  Gs-GPCR agonist  377 nM  Isensee et al., 2014b  
DAMGOc Gi-GPCR agonist  321 nM  Isensee et al., 2017a  
Fentanyl Gi-GPCR agonist  97 nM 36 nM Isensee et al., 2017a  
Fsk Activator  1.7 µM 2.6 µM Isensee et al., 2014a, 2017a  
Sp-8-Br-cAMPS Activator 1.66 203 µM  This study 
Sp-8-Br-cAMPS-AM Activator  1.3 µM 6.8 µM Isensee et al., 2014a, 2017a  
Rp-cAMPS Inhibitor 1.21   Schwede et al., 2015  
Rp-cAMPS-pAB Inhibitor  ∼10 µM  This study 
Rp-8-pCPT-cAMPS Inhibitor 2.72   This study 
Rp-8-pCPT-cAMPS-pAB Inhibitor  ∼4 µM  This study 
Rp-8-Br-cAMPS Inhibitor 1.47   This study 
Rp-8-Br-cAMPS-pAB Inhibitor  ∼3 µM  This study 
a

Lipophilicity (log K′g values) according to reversed-phase HPLC protocol (Krass et al., 1997).

b

Half maximal effective concentration (EC50) or half maximal inhibitory concentration (IC50) determined using the pRII assay in rat or mouse sensory neurons.

c

DAMGO, [D-Ala2, N-MePhe4, Gly-ol]-enkephalin.

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