Ligand Structural Specificity of GABAA Receptors in Guinea Pig Ileum
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Ligand Structural Specificity of GABAA Receptors in Guinea Pig Ileum. / Kristiansen, Uffe; Fjalland, Bjarne.
In: Pharmacology & Toxicology, Vol. 68, No. 5, 05.1991, p. 332-339.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Ligand Structural Specificity of GABAA Receptors in Guinea Pig Ileum
AU - Kristiansen, Uffe
AU - Fjalland, Bjarne
PY - 1991/5
Y1 - 1991/5
N2 - Abstract: The ligand structural specificity of ileal GABAA receptors was examined using the strength and half‐life of contractions in guinea‐pig myenteric plexus‐longitudinal muscle preparations. The agonists used differ by more than a factor of 1000 in affinity to central GABAA receptors and include both conformationally flexible and restricted molecules as well as pairs of enantiomers. The overall correlation between ileal contractile activity and rat brain receptor affinity was poor (r = 0.75), but within groups of conformationally flexible or conformationally restricted molecules a high correlation was found (r>0.9999). When comparing data for ileal contractile activity with available data for agonist activity in the CNS no difference between ligand specificity of ileal and central GABAA receptors was apparent with the present range of ligands. The half‐lives of ileal contractile responses were found to decrease with increasing GABAB agonist activity 1991 Nordic Pharmacological Society
AB - Abstract: The ligand structural specificity of ileal GABAA receptors was examined using the strength and half‐life of contractions in guinea‐pig myenteric plexus‐longitudinal muscle preparations. The agonists used differ by more than a factor of 1000 in affinity to central GABAA receptors and include both conformationally flexible and restricted molecules as well as pairs of enantiomers. The overall correlation between ileal contractile activity and rat brain receptor affinity was poor (r = 0.75), but within groups of conformationally flexible or conformationally restricted molecules a high correlation was found (r>0.9999). When comparing data for ileal contractile activity with available data for agonist activity in the CNS no difference between ligand specificity of ileal and central GABAA receptors was apparent with the present range of ligands. The half‐lives of ileal contractile responses were found to decrease with increasing GABAB agonist activity 1991 Nordic Pharmacological Society
UR - http://www.scopus.com/inward/record.url?scp=0025732683&partnerID=8YFLogxK
U2 - 10.1111/j.1600-0773.1991.tb01249.x
DO - 10.1111/j.1600-0773.1991.tb01249.x
M3 - Journal article
C2 - 1658764
AN - SCOPUS:0025732683
VL - 68
SP - 332
EP - 339
JO - Pharmacology and Toxicology
JF - Pharmacology and Toxicology
SN - 0901-9928
IS - 5
ER -
ID: 276334075