Abstract：
:The cloned 5-HT3 receptor from NCB-20 neuroblastoma cells was expressed in Xenopus oocytes. In these oocytes, 5-HT, the selective 5-HT3 receptor agonists, 2-methyl-5-HT and m-chlorophenylbiguanide activated an inward current which was sensitive to the specific 5-HT3 receptor antagonist LY278584. Cocaine (0.1 to 10 microM) reversibly inhibited the current activated by 1 microM 5-HT in a concentration-dependent manner. The IC50 value is 0.7 microM and the apparent Hill coefficient is 1.55. This effect of cocaine was not dependent on membrane potential. Cocaine also produced a parallel shift of the 5-HT concentration-response curve to the right and did not reduce the maximal current induced by 5-HT. In the presence of 3 microM cocaine, the EC50 value of 5-HT was increased from 3.08 microM to 6.1 microM. Other local anesthetics such as tricaine and lidocaine also inhibited the current induced by 5-HT. These results suggest that the 5-HT3 receptors expressed in Xenopus oocytes exhibit properties similar to those in sensory neurons and neuroblastoma cells and were blocked by cocaine in a competitive manner.
journal_name
Brain Resjournal_title
Brain researchauthors
Fan P,Oz M,Zhang L,Weight FFdoi
10.1016/0006-8993(94)01316-asubject
Has Abstractpub_date
1995-03-06 00:00:00pages
181-4issue
2eissn
0006-8993issn
1872-6240pii
0006-8993(94)01316-Ajournal_volume
673pub_type
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