The aim of the present study was to evaluate the possible involvement of GABAB receptors in nicotine-induced hypolocomotion and antinociceptive effects in mice. Animals were exposed to nicotine only once. Acute nicotine hydrogen tartrate salt (3mg/kg; subcutaneous, s.c.) administration induced hypolocomotion and antinociceptive responses in the tail-immersion and the hot-plate tests. The effect...

Cui, Lu-Ning, Elaine Coderre, and Leo P. Renaud. GABAB presynaptically modulates suprachiasmatic input to hypothalamic paraventricular magnocellular neurons. Am J Physiol Regulatory Integrative Comp Physiol 278: R1210– R1216, 2000.—This study used whole cell patch clamp recordings in rat hypothalamic slice preparations to evaluate the effects of GABAB receptor activation on GABAA-mediated inhib...

Chronic pain is very difficult to treat. Thus, novel analgesics are a critical area of research. Strong pre-clinical evidence supports the analgesic effects of α-conopeptides, Vc1.1 and RgIA, which block α9α10 nicotinic acetylcholine receptors (nAChRs). However, the analgesic mechanism is controversial. Some evidence supports the block of α9α10 nAChRs as an analgesic mechanism, while other evid...

Tight-seal whole-cell recordings from CA1 pyramidal cells of rodent hippocampus were performed to study GABAB receptor-mediated inhibition of tetrodotoxin (TTX)-resistant IP-SCs. IPSCs were recorded in the presence of TTX and glutamate receptor antagonists. (R)-(-)-baclofen reduced the frequency of TTX-resistant IPSCs by a presynaptic action. The inhibition by (R)-(-)-baclofen was concentration...

N,N -Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6diamine (GS39783) and structurally related compounds are described as novel allosteric enhancers of GABAB receptor function. They potentiate GABA-stimulated guanosine 5 -O-(3-[S]thio)triphosphate ([S]GTP S) binding to membranes from a GABAB(1b/2)-expressing Chinese hamster ovary cell line at low micromolar concentrations, but do not stim...

The present work was performed to show the possible interaction of GAB A, and GABAB receptors in catalepsy. The following results were obtained: 1- Muscimol (MUS), a GABAA agonist, induced catalepsy. This effect was dose-dependent. Baclofen (BAC), a GABAB agonist, had no effect in this respect. 2- Catalepsy induced by muscimol was potentiated by pretreatment of animals with bicuculline (BI...

-Hydroxybutyrate (GHB), a metabolite of -aminobutyric acid (GABA), is an increasingly popular drug of abuse and was recently approved for the treatment of narcolepsy (Xyrem). GHB and GABA receptors have been implicated in mediating effects of GHB; however, the relative importance of each of these receptors is unclear. This study evaluated the effects of selective antagonists in combination with...

Since CXCL12 and its receptors, CXCR4 and CXCR7, have been found in the brain, the role of this chemokine has been expanded from chemoattractant in the immune system to neuromodulatory in the brain. Several pieces of evidence suggest that this chemokine system could crosstalk with the GABAergic system, known to be the main inhibitory neurotransmitter system in the brain. Indeed, GABA and CXCL12...