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Related Experiment Videos

5-HT5 receptors.

D L Nelson1

  • 1Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285-0814, USA. dlgnelson@lilly.com

Current Drug Targets. CNS and Neurological Disorders
|February 18, 2004
PubMed
Summary
This summary is machine-generated.

The 5-HT(5) receptor family, including 5-HT(5A) and 5-HT(5B), is primarily in the CNS. The 5-HT(5A) receptor knockout mice show reduced responses to LSD, highlighting its role.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • The serotonin 5-HT(5) receptor family comprises two subtypes: 5-HT(5A) and 5-HT(5B).
  • 5-HT(5A) receptors are found in humans, mice, and rats, primarily in the central nervous system (CNS), with some presence in the carotid body.
  • 5-HT(5B) receptors are expressed in rodents but absent in humans due to coding sequence interruptions.

Purpose of the Study:

  • To review the current understanding of the 5-HT(5) receptor family.
  • To highlight the limited pharmacological characterization and known functions of these receptors.

Main Methods:

  • Literature review of studies on 5-HT(5A) and 5-HT(5B) receptor distribution and function.
  • Analysis of pharmacological data, including radioligand binding assays using [(125)I]LSD and [(5)H]5-CT.

Related Experiment Videos

  • Examination of findings from 5-HT(5A) receptor knockout mouse models.
  • Main Results:

    • 5-HT(5A) receptors exhibit a broad CNS distribution, while 5-HT(5B) receptors have a restricted distribution.
    • 5-HT(5A) receptors couple to Gi/o proteins, inhibiting adenylyl cyclase activity.
    • LSD shows high affinity for both receptor subtypes, acting as a partial agonist at 5-HT(5A); 5-carboxamidotryptamine (5-CT) also demonstrates high affinity and potency at 5-HT(5A).

    Conclusions:

    • The 5-HT(5A) receptor knockout mice display a blunted locomotor response to LSD.
    • The in vivo role of the 5-HT(5B) receptor remains largely unknown.
    • 5-HT(5) receptors represent some of the least understood serotonin receptor subtypes.