Modulation of agonist and antagonist interactions in serotonin 1A receptors by alcohols.
نویسندگان
چکیده
The serotonin type IA (5-HT1A) receptors are members of a superfamily of seven transmembrane domain receptors that couple to GTP binding regulatory proteins (G-proteins). Serotonergic signalling has been shown to play an important role in alcohol tolerance and dependence. We have studied the effects of alcohols on ligand (agonist and antagonist) binding to bovine hippocampal 5-HT1A receptor in native as well as solubilized membranes. Our results show that alcohols inhibit the specific binding of the agonist OH-DPAT and the antagonist p-MPPF to 5-HT1A receptors in a concentration-dependent manner.
منابع مشابه
Effect of alcohols on G-protein coupling of serotonin(1A) receptors from bovine hippocampus.
The serotonin(1A) (5-hydroxytryptamine [5-HT](1A)) receptors are members of a superfamily of seven transmembrane domain receptors that couple to G-proteins. Serotonergic signalling has been shown to play an important role in alcohol intake, preference and dependence. G-protein coupling of the 5-HT(1A) receptor serves as an important determinant for serotonergic signalling. We have studied the e...
متن کاملPeripheral 5-HT1A and 5-HT7 Serotonergic Receptors Modulate Parasympathetic Neurotransmission in Long-Term Diabetic Rats
We analyzed the modulation of serotonin on the bradycardia induced in vivo by vagal electrical stimulation in alloxan-induced long-term diabetic rats. Bolus intravenous administration of serotonin had a dual effect on the bradycardia induced either by vagal stimulation or exogenous Ach, increasing it at low doses and decreasing it at high doses of 5-hydroxytryptamine (5-HT), effect reproduced b...
متن کاملDifferential discrimination of G-protein coupling of serotonin(1A) receptors from bovine hippocampus by an agonist and an antagonist.
We have studied the effect of guanosine-5'-O-(3-thiotriphosphate) (GTP-gamma-S), a non-hydrolyzable analogue of GTP, on agonist and antagonist binding to bovine hippocampal 5-hydroxytryptamine (5-HT)(1A) receptor in native membranes. Our results show that the specific binding of the agonist is inhibited with increasing concentrations of GTP-gamma-S along with a reduction in binding affinity. In...
متن کاملThe effect of fluoxetine on thermal hyperalgesia in STZ-induced diabetic mice: possible involvement of 5-HT1/2 receptors
Diabetic neuropathic pain, an important micro vascular complication in diabetes mellitus, has been recognized as one of the most difficult types of pain to treat. Lack of understanding of etiology involved, inadequate relief, development of tolerance and potential toxicity of classical anti-nociceptive agents warrants the investigation of newer agents to relieve this pain. The aim of the presen...
متن کاملThe Effect of 5HT3 Agonist Receptor of the Lateral Hippocampal on Amnesia Induce by Morphine in Mice
Background and Objective: It has been shown that the opioidergic system exerts widespread effects on cognitive functions. Interactions between opioid and serotonin receptors have been reported in some brain structures such as the dorsal hippocampus, thus a functional interaction between opioids and serotonin seems possible concerning memory control. The purpose of this study was to assess the e...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- FEBS letters
دوره 438 1-2 شماره
صفحات -
تاریخ انتشار 1998