Regions of beta 4.beta 2 subunit chimeras that contribute to the agonist selectivity of neuronal nicotinic receptors

FEBS Lett. 1992 Aug 24;308(3):245-8. doi: 10.1016/0014-5793(92)81284-s.

Abstract

Fifteen chimeric nicotinic receptor beta subunits were constructed consisting of N-terminal neuronal beta 4 sequences and C-terminal beta 2 sequences. Responses to cytisine, nicotine, or tetramethylammonium were compared to acetylcholine responses for these subunits expressed in Xenopus oocytes with alpha 3 subunits. The results show that (i) two residues in the extracellular domain of chimeric beta 4.beta 2 subunits (108 beta 2F/beta 4V, 110 beta 2S/beta 4T) account for much of the relative cytisine sensitivity; and (ii) four extracellular residues of chimeric beta 4.beta 2 subunits (112 beta 2A/beta 4V, 113 beta 2V/beta 4I and 115 beta 2S/beta 4R, 116 beta 2Y/beta 4S) account for most of the relative tetramethylammonium sensitivity. The data did not permit localization of nicotine sensitivity to any particular region.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acetylcholine / metabolism
  • Alkaloids / metabolism
  • Amino Acid Sequence
  • Animals
  • Azocines
  • DNA Mutational Analysis
  • Molecular Sequence Data
  • Neurons / metabolism*
  • Nicotine / metabolism
  • Oocytes
  • Quaternary Ammonium Compounds / metabolism
  • Quinolizines
  • Receptors, Nicotinic / chemistry*
  • Receptors, Nicotinic / genetics
  • Receptors, Nicotinic / metabolism
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / metabolism
  • Structure-Activity Relationship
  • Xenopus

Substances

  • Alkaloids
  • Azocines
  • Quaternary Ammonium Compounds
  • Quinolizines
  • Receptors, Nicotinic
  • Recombinant Fusion Proteins
  • cytisine
  • Nicotine
  • tetramethylammonium
  • Acetylcholine