Serotonin Receptor Subtypes in Brain: Ligand Binding Properties and Coupling with G Proteins

  • Yasuyuki Nomura
  • Yoshihisa Kitamura
  • Michihisa Tohda
  • Shin-ichi Imai
  • Toshiaki Katada
  • Michio Ui
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 287)


Serotonin (5-hydroxytryptamine; 5-HT) receptors are classified as 5-HT1, 5-HT2 and 5-HT3, and evidence is emerging to suggest heterogeneity within 5-HT1 receptor category, e.g., 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors (Peroutka, 1988). Several GTP-binding proteins (G proteins) in mammalian brain were identified, e.g., α52/45, α41, α40, α39 (α-subunits of Gs, Gi1, Gi2 and Go) (Katada et al., 1986a; Katada et al., 1987; Itoh et al., 1988; Casey and Gliman, 1988) and several G proteins with low molecular weight (20 ~ 30 kDa), including 24-kDa G protein (24 K-G) (Katada and Ui, 1988), ADP-ribosylation factor (ARF) (Kahn and Gliman, 1986), a substrate of botulinum toxin (Gb, rho product) (Narumiya et al., 1988) and other small molecular G proteins (smg) (Takai et al., 1989). N-ethylmaleimide (NEM) has been used as a useful probe to alkylate sulfhydryl residues in receptors and G proteins involved in their coupling (Katada et al., 1986b; Kitamura and Nomura, 1987; Nomura et al., 1988). To classify 5-HT receptor subtypes in the CNS from binding characteristics and the aspect of coupling properties of these receptors with G proteins, we here examined the effects of GTPyS, NEM and several 5-HT receptor ligands on specific binding of [3H]8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) (5-HT1A), [125I]iodocyanopindolol (ICYP) (5-HT1B), [ 3H]mesulergine (5-HT1C), [3H] 4-bromo-2,5-dimethoxyphenyliso-propylamine (DOB) (5-HT2) and [3H]ketanserin (5-HT2) to crude synaptic membranes of rat brain.


Pertussis Toxin Brain Membrane Competition Curve Guanine Nucleotide Regulatory Protein Receptor Clone 
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Copyright information

© Plenum Press, New York 1991

Authors and Affiliations

  • Yasuyuki Nomura
    • 1
  • Yoshihisa Kitamura
    • 1
  • Michihisa Tohda
    • 1
  • Shin-ichi Imai
    • 1
  • Toshiaki Katada
    • 2
  • Michio Ui
    • 3
  1. 1.Department of Pharmacology, Faculty of Pharmaceutical SciencesHokkaido UniversitySapporo 060Japan
  2. 2.Department of Life Science, Faculty of ScienceTokyo Institute of TechnologyYokohama 227Japan
  3. 3.Department of Physiological Chemistry, Faculty of Pharmaceutical SciencesTokyo UniversityTokyo 113Japan

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