Molecular Cloning and Characterization of a Rat Brain cDNA Encoding a 5-hydroxytryptamine1B Receptor

EMBO J. 1991 Dec;10(13):4017-23.

Abstract

To date, there have been at least eight different receptors for the neurotransmitter serotonin (5-HT) identified in the central nervous system. These receptors fall into four pharmacological classes: 5-HT1, 5-HT2, 5-HT3 and 5-HT4. The 5-HT1 class has been shown to contain at least four pharmacologically distinct subtypes, 5-HT1A-D. Of these, cDNAs encoding the 5-HT1A and 5-HT1C receptors have been previously characterized. We now report the cloning and expression of a rat brain cDNA encoding another member of the 5-HT1 receptor family. Transient expression of this clone demonstrated high-affinity binding of [3H]5-HT with a pharmacological profile corresponding to that of the 5-HT1B subtype: 5-CT, 5-HT greater than propranolol greater than methysergide greater than rauwolscine greater than 8-OH-DPAT. In situ hybridization revealed expression of cognate mRNA within cells of the dorsal and median raphe nuclei, consistent with previous reports that the 5-HT1B receptor acts as an autoreceptor on 5-HT terminals in this species. mRNA expression was also detected in cells within the CA1 region of hippocampus, striatum, layer 4 of cortex and in the cerebellum, suggesting a previously unrecognized post-synaptic role for the 5-HT1B receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • Amino Acid Sequence
  • Animals
  • Base Sequence
  • Binding, Competitive
  • Brain / metabolism*
  • Cells, Cultured
  • Cloning, Molecular
  • DNA / genetics*
  • Humans
  • Methysergide / metabolism
  • Molecular Sequence Data
  • Nucleic Acid Hybridization
  • Propranolol / metabolism
  • RNA, Messenger / genetics
  • Radioligand Assay
  • Rats
  • Receptors, Serotonin / classification
  • Receptors, Serotonin / genetics*
  • Receptors, Serotonin / metabolism
  • Sequence Alignment
  • Serotonin / analogs & derivatives
  • Serotonin / metabolism
  • Tetrahydronaphthalenes / metabolism
  • Transfection
  • Yohimbine / metabolism

Substances

  • RNA, Messenger
  • Receptors, Serotonin
  • Tetrahydronaphthalenes
  • Yohimbine
  • Serotonin
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • DNA
  • 5-carboxamidotryptamine
  • Propranolol
  • Methysergide