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Chemical Compound Review:

Lopac-P-9159 piperidine-4-sulfonic acid

Synonyms: CHEMBL34155, P9159_SIGMA, CHEBI:146429, CCG-205104, Lopac0_001024, ...

Curtis, D.R. et al., Wafford, K.A. et al., Miller, J.W. et al., Miller, J.W. et al., Ebert, B. et al., et al.

Wafford, Thompson, Thomas, Sikela, Wilcox, Whiting,

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Disease relevance of piperidine-4-sulfonic acid

Injections of the GABAA-agonist piperidine-4-sulfonic acid and the GABAB-agonist (-)baclofen in the CeM markedly facilitated myoclonic and clonic seizures, but had different effects on tonic seizures [1].

High impact information on piperidine-4-sulfonic acid

GABA affinity seemed to be identical to that of the alpha 1 beta 1 gamma 2 receptor; however, the partial agonists 4,5,6,7-tetrahydroisoxazolo-[5,4-c]pyridin-3-ol and piperidine-4-sulfonic acid showed lower efficacy than at either alpha 1 beta 1 gamma 2 or alpha 6 beta 1 gamma 2 [2].
We have characterized GABA, (RS)-dihydromuscimol, piperidine-4-sulfonic acid, and 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol with recombinant human GABAA receptors expressed in Xenopus oocytes [3].
Brain-stem areas tonically inhibiting dorsal horn neurones: studies with microinjection of the GABA analogue piperidine-4-sulphonic acid [4].
The binding of radioactive piperidine-4-sulphonic acid ([3H]P4S) to thoroughly washed, frozen, and thawed membranes isolated from cow and rat brains has been studied [5].
Effects of bilateral control microinjections in the fastigial (medial) cerebellar nucleus were compared with different doses of the GABAA agonist piperidine-4-sulfonic acid and the GABAB agonist (-)baclofen (Bf) [6].

Anatomical context of piperidine-4-sulfonic acid

When administered microelectrophoretically, GABA and the GABA-mimetic piperidine-4-sulphonic acid (P4S) appear to have no direct hyperpolarizing or depolarizing effect on the terminations of motor axon collaterals excited electrically in the ventral horn of the lumbar spinal cord of the cat [7].

References

The central medial nucleus: thalamic site of seizure regulation. Miller, J.W., Ferrendelli, J.A. Brain Res. (1990) [Pubmed]
Functional characterization of human gamma-aminobutyric acidA receptors containing the alpha 4 subunit. Wafford, K.A., Thompson, S.A., Thomas, D., Sikela, J., Wilcox, A.S., Whiting, P.J. Mol. Pharmacol. (1996) [Pubmed]
Molecular pharmacology of gamma-aminobutyric acid type A receptor agonists and partial agonists in oocytes injected with different alpha, beta, and gamma receptor subunit combinations. Ebert, B., Wafford, K.A., Whiting, P.J., Krogsgaard-Larsen, P., Kemp, J.A. Mol. Pharmacol. (1994) [Pubmed]
Brain-stem areas tonically inhibiting dorsal horn neurones: studies with microinjection of the GABA analogue piperidine-4-sulphonic acid. Foong, F.W., Duggan, A.W. Pain (1986) [Pubmed]
Characterization of the binding of the GABA agonist [3H]piperidine-4-sulphonic acid to bovine brain synaptic membranes. Krogsgaard-Larsen, P., Snowman, A., Lummis, S.C., Olsen, R.W. J. Neurochem. (1981) [Pubmed]
Role of the fastigial nucleus in generalized seizures as demonstrated by GABA agonist microinjections. Miller, J.W., Gray, B.C., Turner, G.M. Epilepsia (1993) [Pubmed]
On the probable absence of GABA receptors on the terminations of motor axon collaterals in the cat spinal cord. Curtis, D.R., Gynther, B.D. Experimental brain research. Experimentelle Hirnforschung. Expérimentation cérébrale. (1986) [Pubmed]

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