The effects of SB 204070, a highly potent and selective 5-HT4 receptor antagonist, on guinea-pig distal colon.

@article{Wardle1994TheEO,
  title={The effects of SB 204070, a highly potent and selective 5-HT4 receptor antagonist, on guinea-pig distal colon.},
  author={Kathryn Wardle and E S Ellis and Gordon S Baxter and Guy A. Kennett and Laramie M. Gaster and Gareth J Sanger},
  journal={British journal of pharmacology},
  year={1994},
  volume={112 3},
  pages={789-94}
}
1. The pharmacology of a novel 5-HT4 receptor antagonist, SB 204070 has been evaluated in the guinea-pig isolated distal colon longitudinal muscle-myenteric plexus (LMMP). 2. SB 204070 is a highly potent antagonist of 5-HT-evoked cholinergically-mediated contractions in the guinea-pig distal colon. Low concentrations (10-100 pM) produced a shift to the right of the curve (apparent pA2 10.8 +/- 0.1) with no significant effect on the maximum response. With higher concentrations of SB 204070 (300… CONTINUE READING

Connections & Topics

Mentioned Connections BETA
MuscleSibling in is aPlexus
The pharmacology of a novel 5-HT4 receptor antagonist , SB 204070 has been evaluated in the guinea - pig isolated distal colon longitudinal muscle - myenteric plexus ( LMMP ) .
PlexusSibling in is aMuscle
The pharmacology of a novel 5-HT4 receptor antagonist , SB 204070 has been evaluated in the guinea - pig isolated distal colon longitudinal muscle - myenteric plexus ( LMMP ) .
MuscleNo subtypePlexus
The pharmacology of a novel 5-HT4 receptor antagonist , SB 204070 has been evaluated in the guinea - pig isolated distal colon longitudinal muscle - myenteric plexus ( LMMP ) .
PlexusNo subtypeMuscle
The pharmacology of a novel 5-HT4 receptor antagonist , SB 204070 has been evaluated in the guinea - pig isolated distal colon longitudinal muscle - myenteric plexus ( LMMP ) .
5 . Radioligand binding studies show that SB 204070 has a greater that 5000 fold selectivity for the 5-HT4 receptor over 5-HT1A , 5-HT1D , 5-HT1E , 5-HT2A , 5-HT2C , 5-HT3 , GABAA , BDZ , TBPS , A1 adenosine receptors , alpha 1 , alpha 2 , beta 1 , beta 2 adrenoceptors and D1 , D2 and D3 dopamine receptors .
5 . Radioligand binding studies show that SB 204070 has a greater that 5000 fold selectivity for the 5-HT4 receptor over 5-HT1A , 5-HT1D , 5-HT1E , 5-HT2A , 5-HT2C , 5-HT3 , GABAA , BDZ , TBPS , A1 adenosine receptors , alpha 1 , alpha 2 , beta 1 , beta 2 adrenoceptors and D1 , D2 and D3 dopamine receptors .
The antagonism seen with SB 204070 is unlikely to be due to a non - selective effect since high concentrations ( 10 nM and 1 microM ) of the compound had no effect on cholinergically - mediated contractions evoked by the nicotinic receptor agonist , DMPP , in the same preparation .
All Topics