title: 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.
abstract: 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-β-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.
authors.forename: Jingxia
authors.initials: J
authors.lastname: Yue
authors.forename: Yi
authors.initials: Y
authors.lastname: Zhang
authors.forename: Xuemin
authors.initials: X
authors.lastname: Li
authors.forename: Shan
authors.initials: S
authors.lastname: Gong
authors.forename: Jin
authors.initials: J
authors.lastname: Tao
authors.forename: Xinghong
authors.initials: X
authors.lastname: Jiang
mesh_terms: D000818:Animals; D020747:Calcium Channels, T-Type / Q000187:drug effects*; D002772:Cholera Toxin / Q000494:pharmacology*; D017868:Cyclic AMP-Dependent Protein Kinases / Q000378:metabolism*; D005260:Female; D008564:Membrane Potentials / Q000187:drug effects; D053858:Metabolic Networks and Pathways / Q000187:drug effects; D051379:Mice; D008813:Mice, Inbred ICR; D009474:Neurons / Q000187:drug effects*; D018408:Patch-Clamp Techniques; D011960:Receptors, Estrogen; D043562:Receptors, G-Protein-Coupled / Q000187:drug effects / Q000378:metabolism*; D012668:Trigeminal Ganglion / Q000166:cytology / Q000187:drug effects*
chemical_list: D020747:Calcium Channels, T-Type; C532507:GPER1 protein, mouse; D011960:Receptors, Estrogen; D043562:Receptors, G-Protein-Coupled; D002772:Cholera Toxin; D017868:Cyclic AMP-Dependent Protein Kinases