Exploring the pharmacological properties of insect nicotinic acetylcholine receptors

被引：128
作者：
Thany, Steeve H.
Lenaers, Guy
Raymond-Delpech, Valerie
Sattelle, David B.
Lapied, Bruno
机构：
[1] Univ Angers, UFR Sci, Lab Recepteurs & Canaux Ion Membranaires, INRA,USC,UPRES EA 2467, F-49045 Angers, France
[2] Univ Montpellier, Inst Neurosci Montpellier, INSERM, U583,IFR76, F-34091 Montpellier, France
[3] Univ Toulouse 3, CRCA, CNRS, UMR 5169, F-31062 Toulouse, France
[4] Univ Oxford, Dept Physiol Anat & Genet, MRC, Funct Genet Unit, Oxford OX1 3QX, England
来源：
TRENDS IN PHARMACOLOGICAL SCIENCES | 2007年 / 28卷 / 01期
基金：
英国医学研究理事会;
关键词：
XENOPUS-LAEVIS OOCYTES; ALPHA-BUNGAROTOXIN; APIS-MELLIFERA; FUNCTIONAL EXPRESSION; KENYON CELLS; GENE FAMILY; MOLECULAR CHARACTERIZATION; DROSOPHILA-MELANOGASTER; MAMMALIAN-CELLS; HIGH-AFFINITY;
D O I：
10.1016/j.tips.2006.11.006
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Insect nicotinic acetylcholine (nACh) receptors are molecular targets of insecticides such as neonicotinoids that are used to control disease-carrying insects and agricultural pests. To date, several insect nACh receptor subunits have been identified, indicating different nACh receptor subtypes and pharmacological profiles. Because of the difficulty in expressing functional insect nACh receptors in heterologous systems, new research tools are needed. Studies on insects resistant to the insecticide imidacloprid and on laboratory-generated hybrid and chimaeric nACh receptors in vitro have provided information about the molecular basis of receptor diversity, neonicotinoid resistance and selectivity. Additionally, recent results indicate that the sensitivity of insect nACh receptors to imidacloprid can be modulated by intracellular phosphorylation mechanisms, which offers a new approach to studying insect nACh receptor pharmacology.
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收藏
页码：14 / 22
页数：9
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