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Table 1 Effects of GSNO treatment on agonist dose-response parameters in [35S]GTPγS binding assays of various Gi-coupled receptors in their native cellular environment. Membranes or lysates were preincubated in control conditions or in the presence of 0.5 mM GSNO for 30 min. Values are mean ± SE from three to four independent experiments performed in duplicate. Emax is expressed in percentage over basal with nonspecific binding subtracted.

From: S-Nitrosothiols modulate G protein-coupled receptor signaling in a reversible and highly receptor-specific manner

 

Control

GSNO

Receptor (agonist)

log(EC50)

Emax (%)

log(EC50)

Emax (%)

Rat forebrain membranes

    

M2/M4 mAChRs (CCh)

-4.94 ± 0.05

176 ± 2

-5.55 ± 0.11**

207 ± 4**

LPA1 (LPA)

-6.84 ± 0.26

140 ± 7

-6.53 ± 0.40

116 ± 3*

Cannabinoid CB1 (CP55940)

-7.84 ± 0.07

223 ± 3

-7.69 ± 0.08

183 ± 2***

Adenosine A1 (2ClAdo)

-6.90 ± 0.04

256 ± 3

-6.87 ± 0.12

234 ± 7*

μ-opiate (DAMGO)

-6.85 ± 0.09

167 ± 3

-7.31 ± 0.19

164 ± 5

ORL1 (Nociceptin)

-8.66 ± 0.12

173 ± 3

-8.78 ± 0.10

161 ± 2*

CHO cell lysates

    

LPA (LPA)

-7.37 ± 0.11

202 ± 4

-7.05 ± 0.12

176 ± 4**

Human platelet membranes

    

P2Y12 (MeSADP)

-8.19 ± 0.03

279 ± 2

-8.30 ± 0.08

195 ± 3***

α2A-adrenoceptor (NA)

-5.33 ± 0.08

161 ± 2

-5.49 ± 0.09

182 ± 3**

  1. * Statistically different from control (P < 0.05)
  2. ** Statistically different from control (P < 0.01)
  3. *** Statistically different from control (P < 0.001)