PMID- 25985574
OWN - NLM
STAT- MEDLINE
DCOM- 20150602
LR  - 20191126
IS  - 0031-7144 (Print)
IS  - 0031-7144 (Linking)
VI  - 69
IP  - 11
DP  - 2014 Nov
TI  - Activation of G-protein-coupled receptor 30 increases T-type calcium currents in 
      trigeminal ganglion neurons via the cholera toxin-sensitive protein kinase A 
      pathway.
PG  - 804-8
AB  - G protein-coupled receptor 30 (GPR30) is a seven transmembrane domain G protein 
      coupled receptor. In our study, GPR30 expression was found in trigeminal ganglia 
      (TG) in mice, detected by RT-PCR and western blotting. We examined the effects of 
      GPR30 activation on T-type calcium channels using GPR30-specific compound 1 
      (G-1), a GPR30-selective agonist, in TG neurons and demonstrated that G-1 induced 
      an increase in T-type calcium channel currents (T-currents) in TGs. Intracellular 
      infusion of GDP-beta-S and pre-treatment of the neurons with cholera toxin (CTX) 
      blocked the effects of G-1, suggesting that the G(s)-protein was involved. 
      Intracellular application of the protein kinase A (PKA) inhibitor PKI 6-22 or 
      pretreatment of the neurons with H89 abolished G-1 -induced enhancement of 
      T-currents in TG neurons. However, incubation with PKC inhibitor elicited no such 
      effects. In conclusion, our study shows that activation of GPR30 by G-1 increases 
      T-currents via the CTX-sensitive and PKA-dependent pathway.
FAU - Yue, Jingxia
AU  - Yue J
FAU - Zhang, Yi
AU  - Zhang Y
FAU - Li, Xuemin
AU  - Li X
FAU - Gong, Shan
AU  - Gong S
FAU - Tao, Jin
AU  - Tao J
FAU - Jiang, Xinghong
AU  - Jiang X
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Germany
TA  - Pharmazie
JT  - Die Pharmazie
JID - 9800766
RN  - 0 (Calcium Channels, T-Type)
RN  - 0 (GPER1 protein, mouse)
RN  - 0 (Receptors, Estrogen)
RN  - 0 (Receptors, G-Protein-Coupled)
RN  - 9012-63-9 (Cholera Toxin)
RN  - EC 2.7.11.11 (Cyclic AMP-Dependent Protein Kinases)
SB  - IM
MH  - Animals
MH  - Calcium Channels, T-Type/*drug effects
MH  - Cholera Toxin/*pharmacology
MH  - Cyclic AMP-Dependent Protein Kinases/*metabolism
MH  - Female
MH  - Membrane Potentials/drug effects
MH  - Metabolic Networks and Pathways/drug effects
MH  - Mice
MH  - Mice, Inbred ICR
MH  - Neurons/*drug effects
MH  - Patch-Clamp Techniques
MH  - Receptors, Estrogen
MH  - Receptors, G-Protein-Coupled/drug effects/*metabolism
MH  - Trigeminal Ganglion/cytology/*drug effects
EDAT- 2015/05/20 06:00
MHDA- 2015/06/03 06:00
CRDT- 2015/05/20 06:00
PHST- 2015/05/20 06:00 [entrez]
PHST- 2015/05/20 06:00 [pubmed]
PHST- 2015/06/03 06:00 [medline]
PST - ppublish
SO  - Pharmazie. 2014 Nov;69(11):804-8.