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Literature DB >> 2986036

[3H](-)Baclofen: an improved ligand for GABAB sites.

Abstract

[3H](-)Baclofen, the radiolabelled form of the active isomer of baclofen, has been used as a ligand for GABAB (gamma-aminobutyric acid) receptors on synaptic membranes from whole brain of rat. The pharmacological profile for displacement of this ligand was observed to be identical with that for the racemic ligand [3H](+/-)baclofen and [3H]GABA under conditions where GABAB, but not GABAA sites, were labelled. The displaceable (specific) portion of membrane-bound [3H](-)baclofen was 47.5 +/- 2.3% of the total which was twice that obtained previously with [3H](+/-)baclofen. Two binding components were observed with affinities of 19 and 304 nM and binding capacities of 0.37 and 1.58 pmol/mg protein respectively. It is suggested that [3H](-)baclofen is an improvement over the labelled racemic form and binds to the same sites. It should provide a more reliable tool for studying GABAB receptors.

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Year: 1985 PMID： 2986036 DOI： 10.1016/0028-3908(85)90075-9

Source DB: PubMed Journal: Neuropharmacology ISSN： 0028-3908 Impact factor: 5.250

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Cited

13 in total

1. The effects of baclofen on calcium channel currents in dorsal sensory cells of the spinal cord in the lamprey.

Authors: I V Batueva; J T Buchanan; E A Tsvetkov; A K Sagatelyan; N P Veselkin
Journal: Neurosci Behav Physiol Date: 1999 Jan-Feb

2. Changes in rectal temperature and ECoG spectral power of sensorimotor cortex elicited in conscious rabbits by i.c.v. injection of GABA, GABA(A) and GABA(B) agonists and antagonists.

Authors: Maria Frosini; Massimo Valoti; Giampietro Sgaragli
Journal: Br J Pharmacol Date: 2003-12-08 Impact factor: 8.739

3. The effects of baclofen on spinal and supraspinal micturition reflexes in rats.

Authors: C A Maggi; P Santicioli; S Giuliani; M Furio; B Conte; P Meli; L Gragnani; A Meli
Journal: Naunyn Schmiedebergs Arch Pharmacol Date: 1987-08 Impact factor: 3.000

4. Effects of pentobarbital tolerance to and dependence on GABAB receptor-binding.

Authors: T Kimura; P A Saunders; I Yamamoto; I K Ho
Journal: Neurochem Res Date: 1991-10 Impact factor: 3.996

5. Interactions of taurine and structurally related analogues with the GABAergic system and taurine binding sites of rabbit brain.

Authors: Maria Frosini; Casilde Sesti; Stefania Dragoni; Massimo Valoti; Mitri Palmi; Henry B F Dixon; Fabrizio Machetti; Giampietro Sgaragli
Journal: Br J Pharmacol Date: 2003-03 Impact factor: 8.739

[3H](-)Baclofen: an improved ligand for GABAB sites.

1. The effects of baclofen on calcium channel currents in dorsal sensory cells of the spinal cord in the lamprey.

2. Changes in rectal temperature and ECoG spectral power of sensorimotor cortex elicited in conscious rabbits by i.c.v. injection of GABA, GABA(A) and GABA(B) agonists and antagonists.

3. The effects of baclofen on spinal and supraspinal micturition reflexes in rats.

4. Effects of pentobarbital tolerance to and dependence on GABAB receptor-binding.

5. Interactions of taurine and structurally related analogues with the GABAergic system and taurine binding sites of rabbit brain.

6. Carrier-mediated transport of baclofen across monolayers of bovine brain endothelial cells in primary culture.

7. MDL 26,479: a potential cognition enhancer with benzodiazepine inverse agonist-like properties.

8. MDL 27,531 selectively reverses strychnine-induced seizures in mice.

9. Systemic baclofen stimulates gastric motility and secretion via a central action in the rat.

10. Facilitation of amphetamine-induced hypothermia in mice by GABA agonists and CCK-8.