Effects of the arylaminopyridazine-GABA derivatives, sr95103 and SR95531 on the Ascaris muscle GABA receptor: the relative potency of the antagonists in Ascaris is different to that at vertebrate GABA, receptors
- Resource Type
- Authors
- A.H. Duittoz; Richard J. Martin
- Source
- Comparative Biochemistry and Physiology-Part C: Comparative Pharmacology
Comparative Biochemistry and Physiology-Part C: Comparative Pharmacology, Elsevier, 1991, 98 (2-3), pp.417-422. ⟨10.1016/0742-8413(91)90227-K⟩
- Subject
- medicine.medical_specialty
[SDV]Life Sciences [q-bio]
Immunology
Pharmacology
03 medical and health sciences
0302 clinical medicine
GABA receptor
Internal medicine
medicine
Receptor
Ascaris suum
030304 developmental biology
0303 health sciences
[SDV.BA.MVSA]Life Sciences [q-bio]/Animal biology/Veterinary medicine and animal Health
biology
GABAA receptor
Ascaris
Antagonist
[SDV.BDLR]Life Sciences [q-bio]/Reproductive Biology
biology.organism_classification
Schild regression
Endocrinology
nervous system
[SDV.NEU]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC]
Antagonism
030217 neurology & neurosurgery
- Language
- English
- ISSN
- 0306-4492
1. GABA-induced changes in input conductance in the bag region of Ascaris suum muscle were monitored using a two-microelectrode current-clamp technique. 2. Effects of the arylaminopyridazine-GABA derivatives, SR95103 and SR95531 on GABA conductance responses were observed. 3. SR95103 was more potent than SR95531 as an antagonist; this potency order contrasts with vertebrate GABA, receptors. 4. The antagonism of SR95103 was associated with a parallel shift to the right in the GABA dose-response relationships. 5. A modified Schild plot was used to describe the action of SR95103: the data was consistent with 2 molecules of GABA but one molecule of antagonist interacting with the receptor. 6. The K B for SR95103 was 64 ± 13 μM (mean ± SE, N = 14).