کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
5560846 1562034 2017 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Pharmacological characterization of histamine-gated chloride channels from the housefly Musca domestica
موضوعات مرتبط
علوم زیستی و بیوفناوری علوم محیط زیست بهداشت، سم شناسی و جهش زایی
پیش نمایش صفحه اول مقاله
Pharmacological characterization of histamine-gated chloride channels from the housefly Musca domestica
چکیده انگلیسی


- Histamine-gated Cl− channels from houseflies were expressed in oocytes.
- HCLB channels are more sensitive to agonists than HCLA channels.
- Besides histamine, GABA and biogenic amines act as HCLB channel agonists.
- Serotonin and dopamine act as competitive HCLB channel antagonists.
- HCLB channels are insensitive to known ligand-gated Cl− channel insecticides.

The biogenic amine histamine (HA) is not only the neurotransmitter of photoreceptors but also has important roles in mechanosensory reception, temperature preference, sleep and olfactory processing in insects. Two cDNAs (MdhclA and MdhclB) that encode HA-gated chloride channel subunits (MdHCLA and MdHCLB) were cloned from the housefly Musca domestica. The cRNAs were injected into Xenopus laevis oocytes to examine the functions and pharmacological characteristics of MdHCLA and MdHCLB channels using a two-electrode voltage clamp method. HA was used to activate MdHCLA and MdHCLB channels to evoke inward currents with EC50s of 33.1 μM and 6.28 μM, respectively. 2-(3-Trifluoromethylphenyl)histamine, an HA H1 receptor agonist, was a partial agonist of MdHCLB receptors with an EC50 of 49.4 μM. MdHCLB channels were also activated by γ-aminobutyric acid (GABA) and monoamines, such as octopamine, serotonin (5-HT) and dopamine (DA); 5-HT and DA also acted as competitive antagonists. GABA acted as a full agonist of MdHCLB receptors with an EC50 of 1.11 mM. d-Tubocurarine, cimetidine and picrotoxinin were poor inhibitors of HA- and GABA-evoked currents in MdHCLB channels. Our data show that HCLB channels are more sensitive to agonists when compared with HCLA channels. HCLB channels are also affected by antagonists but insusceptible to known insecticides that target GABA- and glutamate-gated chloride channels.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: NeuroToxicology - Volume 60, May 2017, Pages 245-253
نویسندگان
, , , , ,