Ligand Structural Specificity of GABAA Receptors in Guinea Pig Ileum

Research output: Contribution to journal › Journal article › Research › peer-review

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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

Harvard

Kristiansen, U & Fjalland, B 1991, 'Ligand Structural Specificity of GABAA Receptors in Guinea Pig Ileum', Pharmacology & Toxicology, vol. 68, no. 5, pp. 332-339. https://doi.org/10.1111/j.1600-0773.1991.tb01249.x

APA

Kristiansen, U., & Fjalland, B. (1991). Ligand Structural Specificity of GABAA Receptors in Guinea Pig Ileum. Pharmacology & Toxicology, 68(5), 332-339. https://doi.org/10.1111/j.1600-0773.1991.tb01249.x

Vancouver

Kristiansen U, Fjalland B. Ligand Structural Specificity of GABAA Receptors in Guinea Pig Ileum. Pharmacology & Toxicology. 1991 May;68(5):332-339. https://doi.org/10.1111/j.1600-0773.1991.tb01249.x

Author

Kristiansen, Uffe ; Fjalland, Bjarne. / Ligand Structural Specificity of GABAA Receptors in Guinea Pig Ileum. In: Pharmacology & Toxicology. 1991 ; Vol. 68, No. 5. pp. 332-339.

Bibtex

@article{bdb765ccb3bb49c68d9020a65cdc2d99,
title = "Ligand Structural Specificity of GABAA Receptors in Guinea Pig Ileum",
abstract = "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",
author = "Uffe Kristiansen and Bjarne Fjalland",
year = "1991",
month = may,
doi = "10.1111/j.1600-0773.1991.tb01249.x",
language = "English",
volume = "68",
pages = "332--339",
journal = "Pharmacology and Toxicology",
issn = "0901-9928",
publisher = "Munksgaard ",
number = "5",

}

RIS

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