The present study was designed to characterise the analgesia produced by the GABA B agonist baclofen in tonic pain in monkeys. The effect of various doses of baclofen was studied on formalin induced pain. Baclofen was injected intraperitoneally 30 min prior to formalin injection in five doses of 2, 4, 6, 8, and 10 mg/kg and the pain was quantified for a period of one hour. Baclofen produced dos...

The relative bioavailability of the test (generic) product 2 × 25 mg baclofen tablets, with respect to the reference product, Lioresal® 2 × 25 mg tablets (baclofen; Squibb) was determined in a single-blind, single dose, randomised, crossover study. The mean values for the variable Cmax were 737.6 ng/ml for the reference and 739.5 ng/ml for the test product. The mean values for the variable AUC ...

AIMS Gamma-aminobutyric acid (GABA)-ergic transmission plays an important role in modulating reinforcing effects of different drugs of misuse. In particular, stimulation of GABA(B) receptors negatively influences self-administration of cocaine, heroin, nicotine, alcohol and gamma-hydroxybutyric acid. The effect and specificity of the GABA(B) agonist baclofen on nicotine misuse were studied on t...

Baclofen is the P-chlorophenyl derivative of gamma-aminobutyric acid (GABA) derivative with an antispasmodic action and is used as a central acting muscle relaxant. GABA is a suppressive neurotransmitter widely distributed in the peripheral and central nervous systems (1). Baclofen [3-(p-Chlorophenyl)4-aminobutanoic acid], is a GABA B agonist. Baclofen has both presynaptic and post synaptic act...

This experiment examined the separate and combined effects of baclofen (5.0 mg/kg, i.p.), a GABA B receptor agonist, and ethanol (2.0 g/kg, i.p.) on flash-evoked potentials (FEPs) recorded from both the visual cortex and superior colliculus (SC) of chronically implanted male Long-Evans rats. In the visual cortex, ethanol significantly decreased the amplitude of positive component P87, but incre...

BACKGROUND Baclofen is a centrally acting gamma-aminobutyric acid agonist used for the symptomatic relief of skeletal muscle spasm and spasticity in traumatic spinal cord lesions, multiple sclerosis, cerebral palsy, and stroke. It is also used in the treatment of chronic hiccups and cocaine abuse. Baclofen-induced central nervous system depression is rare at the usual therapeutic doses. However...

The effects of baclofen, a gamma-amino-n-butyric acid receptor B agonist, on gastric carcinogenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine and how its effects are influenced by selective (M1) and non-selective (M1 and M2) pharmacological blockade of muscarinic receptors were investigated in inbred Wistar rats. Rats were given s.c. injections of 8 mg/kg body wt baclofen with and without...