Cookies Policy

This site uses cookies. By continuing to browse the site you are agreeing to our use of cookies.

I accept this policy

Find out more here

Effects of tandospirone, a novel anxiolytic agent, on human 5-HT1A receptors expressed in Chinese hamster ovary cells (CHO cells)

No metrics data to plot.
The attempt to load metrics for this article has failed.
The attempt to plot a graph for these metrics has failed.
The full text of this article is not currently available.

Brill’s MyBook program is exclusively available on BrillOnline Books and Journals. Students and scholars affiliated with an institution that has purchased a Brill E-Book on the BrillOnline platform automatically have access to the MyBook option for the title(s) acquired by the Library. Brill MyBook is a print-on-demand paperback copy which is sold at a favorably uniform low price.

Access this article

+ Tax (if applicable)
Add to Favorites
You must be logged in to use this functionality

image of Biogenic Amines

Tandospirone is a novel anxiolytic agent which selectively binds to 5-HT1A receptors. In this study, we established a stable CHO cell line expressing human 5-HT1A receptors and examined the action of tandospirone in this cell line. The human 5-HT1A receptor gene was transfected into CHO cells. Several clones showed specific binding of [3H]8-OH-DPAT and one (5HT1A/CHO-No.5) with high density of 5-HT1A receptors was isolated. Scatchard analysis revealed the dissociation constant (Kd) for [3H]8-OH-DPAT of 2.8 nM and the expression level (Bmax) of 956 fmol/mg protein. Competition experiments of [3H]8-OH-DPAT binding showed that affinities (Ki) of several compounds to human 5-HT1A receptors were as follows; 5-HT (8.8 nM), 8-OH-DPAT (3.9 nM), tandospirone (72 nM) buspirone (32 nM), WAY-100635 (0.22 nM) and ritanserin (IC50 > 1 μM). 5-HT, 8-OH-DPAT and tandospirone (0.1 nM–10 μM) concentration-dependently stimulated [35S]GTPγS binding in 5-HT1A/CHO-No.5 cells, but WAY-100635 (10 nM–10 μM) did not. Furthermore, treatment with 5-HT, 8-OH-DPAT, tandospirone and buspirone (0.1 nM–10 μM), but not WAY-100635 (10 nM–10 μM), inhibited forskolin-induced cAMP production in a concentration-dependent manner. These findings suggest that 5-HT1A/CHO-No.5 cells retain 5-HT1A receptor and Gi/o-protein coupling and that tandospirone acts as an agonist at human 5-HT1A receptors.


Full text loading...


Data & Media loading...

Article metrics loading...



Can't access your account?
  • Tools

  • Add to Favorites
  • Printable version
  • Email this page
  • Subscribe to ToC alert
  • Get permissions
  • Recommend to your library

    You must fill out fields marked with: *

    Librarian details
    Your details
    Why are you recommending this title?
    Select reason:
    Biogenic Amines — Recommend this title to your library
  • Export citations
  • Key

  • Full access
  • Open Access
  • Partial/No accessInformation