Nicotinic receptors antagonists

Lobeline. The alkaloid lobehne, whose mechanism of action in unclear but that appears to have dopamine reuptake blockade and nicotinic receptor antagonist properties (Dwoskin and Crooks 2002), was evaluated in a double-bhnd, randomized, placebo-controUed, multicenter trial involving 180 ciga-... 

Brain activity changes (measnred with fMRl) during cigarette withdrawal were recently reported for nicotine-dependent rats (Shoaib et al. 2004). In this study, subcutaneous mecamylamine (1 mg kg ), a nicotine receptor antagonist, was administered to precipitate withdrawal dnring scanning, and this state was compared to a control state after subcntaneons saline administration. After subcutaneous mecamylamine, nicotine-dependent rats had bilateral increases in NAc activity compared to the control state. 

Mecamylamine (a nicotinic receptor antagonist) Mecamylamine decreased intravenous nicotine self-administration under various procedures in rats and monkeys... 

Grabus SD, Martin BR, Brown SE, Damaj MI (2006) Nicotine place preference in the mouse influences of prior handling, dose and strain and attenuation by nicotinic receptor antagonists. Psychopharmacology 184 456 63... 

The dependence indnced by nicotine infnsion can be prevented by coinfusion with the nicotinic receptor antagonist mecamylamine (Malin 2001). 

Most of the anticholinergic drugs which cause delirium have prominently antimuscarinic actions. However, nicotinic receptors are also present in the brain. Mecamylamine, a nicotinic receptor antagonist which penetrates the brain to some extent, has produced delirium (Paykel et al., 1982). Furthermore, general (inhalational) anaesthetics, which by definition decrease arousal, target nicotinic receptors among others (Chapter 9). Conversely, nicotine itself increases arousal and selective attention (Ashton, 1992b). 

A young man broke his leg in a skiing accident, causing severe muscular spasm that necessitated relaxation of the muscle with a competitive nicotinic receptor antagonist before the fracture could be set. At the end of the orthopaedic procedure, the doctor restored neuromuscular transmission by administering ... 

Bisbenzylisoquinolines (macrocyclic or linear, formed by 2 benzylisoquinolines) (+)-tubocurarine (macrocyclic) (acetylcholine (nicotinic) receptor antagonist and skeletal muscle relaxant major component of Chondrodendron species (Menispermaceae) pareira bark-derived curare arrow poison) dauricine (linear) (Menispermaceae curarelike anaesthetic) rodiasine (macrocyclic) (Ocotoea venenosa (Lauraceae) curare-like skeletal muscle relaxant) cepharanthine (macrocyclic) (Stephania species (Menispermaceae) anti-mycobacterial active against leprosy and tuberculosis). 

Acetylcholine receptors provide another target for chemicals with neurotoxic potential most of these act as antagonists. o-Tubocurarine is the classical nicotinic receptor antagonist, and curare-like substances are found in elapid and hydrophid snakes (a-neuro-toxins) such as cobra (a-cobratoxin) and krait... 

Although a wide range of drugs are used to ameliorate symptoms of autistic behavior, currently there is no effective treatment. We discuss novel treatments such as use of cholinesterase inhibitors and nicotinic receptor antagonists as intervention therapies for treatment of the cognitive and non-cognitive changes in the autistic spectrum disorders. 

Wu H-Q, Pereira EFR, Bruno JP, Pellicciari R, Albuquerque EX, Schwarcz R (2010) The astrocyte-derived a7 nicotinic receptor antagonist kynurenic acid controls extracellular glutamate levels in the prefrontal cortex. J Mol Neurosci 40 204-210... 

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