Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo
- S. Hegde, A. Choppin, R. Eglen
- Biology, ChemistryBritish Journal of Pharmacology
- 1 April 1997
In urethane‐anaesthetized rats, the cholinergic component of volume‐induced bladder contractions was inhibited by muscarinic antagonists but had marginal effects on pinacidil‐induced, adenosine 3′:5′‐cyclic monophosphate (cyclic AMP)‐independent, relaxation, consistent with a major contribution of M2 receptors in the generation of volume-induced bladdercontractions.
The interaction of RS 25259‐197, a potent and selective antagonist, with 5‐HT3 receptors, in vitro
A series of isoquinolines have been identified as 5‐HT3 receptor antagonists and competition studies in NG‐108‐15 cells indicated a pharmacological specificity entirely consistent with labelling a 5‐ HT3 receptor, i.e. RS 25259‐197 > granisetron > (S)‐zacopride > tropisetrons.
[3H]BIMU-1, a 5-hydroxytryptamine3 receptor ligand in NG-108 cells, selectively labels sigma-2 binding sites in guinea pig hippocampus.
- D. Bonhaus, D. Loury, E. Wong
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 November 1993
[3H]BIMU-1, under appropriate experimental conditions, is thus the first sigma-2 binding site radioligand to be characterized and may be the first to selectively labels sigma -2 binding sites in guinea pig hippocampus.
Assessment of imiloxan as a selective α2B‐adrenoceptor antagonist
- A. Michel, D. Loury, R. Whiting
- Biology, Chemistry
- 1 March 1990
Imiloxan was identified as a selective α2B ligand while benoxathian displayed a high degree of selectivity for the α2A‐adrenoceptor binding site, which should make it a valuable tool in the classification of α2‐ad Renoceptor subtypes.
Characterization of the muscarinic receptor in isolated uterus of sham operated and ovariectomized rats
- A. Choppin, G. Stepan, D. Loury, N. Watson, R. Eglen
- BiologyBritish Journal of Pharmacology
- 1 August 1999
The pharmacological profile and proportions of the two populations of muscarinic receptors are unaffected by ovariectomy and Radioligand binding experiments indicate the presence of M2 receptors, in addition to M3 receptors, which probably explains the discrepancies between functional and binding affinities.
Identification of a single α1‐adrenoceptor corresponding to the α1A‐subtype in rat submaxillary gland
- A. Michel, D. Loury, R. Whiting
- Biology, Chemistry
- 1 November 1989
Spiperone exhibited 12.9 fold higher affinity for rat liver α1B‐adrenoceptors than for rat submaxillary gland α1A‐ adrenoceptor and may therefore represent the first α1 B‐ad Renoceptor selective ligand.
[3H]RS-23597-190, a potent 5-hydroxytryptamine4 antagonist labels sigma-1 but not sigma-2 binding sites in guinea pig brain.
- D. Bonhaus, D. Loury, E. Wong
- Chemistry, BiologyJournal of Pharmacology and Experimental…
- 1 October 1994
These studies provide additional insight into the structure/affinity relationship of ligands at specific sigma binding sites, and they uncover a novel sigma-1 receptor ligand whose binding is insensitive to the action of phenytoin.
The β1 Sodium Channel Subunit Modifies the Interactions of Neurotoxins and Local Anesthetics with the Rat Brain IIA α Sodium Channel in Isolated Membranes but not in Intact Cells
- D. Bonhaus, R. Herman, J. Hunter
- BiologyNeuropharmacology
- 1 May 1996
Identification of a single alpha 1-adrenoceptor corresponding to the alpha 1A-subtype in rat submaxillary gland.
- A. Michel, D. Loury, R. Whiting
- Biology, ChemistryBritish Journal of Pharmacology
- 1989
The rat liver and submaxillary gland membrane preparations both possessed homogeneous populations of alpha 1-adrenoceptors and there were pharmacological differences between the receptors in these two preparations, suggesting that these receptors were of the alpha 1B-subtype.
Effects of chronic exposure to aflatoxin B1 and aflatoxin M1 on the in vivo covalent binding of aflatoxin B1 to hepatic macromolecules.
The results suggest that the induction of detoxification enzymes following chronic exposure to aflatoxin might contribute to the reduction in covalent binding of AFB1 to macromolecules.
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