Sensitivity of α-conotoxin TxID on stoichiometry of α3β4 nicotinic acetylcholine receptors
- Author:
Dong-Ting ZHANGSUN
1
Author Information
- Publication Type:Journal Article
- Keywords: Different stoichiometry of α and β subunits; Oocytes of Xenopuslaevis; Potency sensitivity; α-conotoxin TxID; α3β4 nAChRs
- From: Chinese Pharmaceutical Journal 2016;51(10):802-808
- CountryChina
- Language:Chinese
- Abstract: OBJECTIVE: To interrogate differential sensitivity of α-conotoxin TxID on stoichiometry of α3β4 nicotinic acetylcholine receptors(nAChRs). METHODS: Oocytes of Xenopus laevis were used to express rat α3β4 nAChRs with different stoichiometries by altering α3:β4 RNA injection ratios of 1:1, 1:10 or 10:1. Sensitivity of α-conotoxin TxID on these different stoichiometry receptors were evaluated and compared. RESULTS: The three stoichiometry receptors of α3β4 nAChRs were expressed in oocytes successfully. α-Conotoxin TxID showed differential sensitivity on α3β4 nAChR stoichiometries. Inhibition of 1:10 injection ratio by TxID was similar with regular 1:1 α3β4 nAChRs within 2-fold difference. While potency of 10:1 injection ratio by TxID decreased 5-fold significantly comparing with 1:1 α3β4 nAChRs. CONCLUSION: α-Conotoxin TxID exhibits distinct sensitivity on different stoichiometry of α3β4 nAChRs, which could reflecting different stoichiometries of α and β subunits. The RESULTS would be helpful for elucidation of structure and physiology function of α3β4 nAChRs.
