Abstract: This application provides a method for the use of select quaternary ammonium antagonists to alpha-7 nAChR for the treatment of cancer and HIV and AIDS.

Abstract: Provided are bis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.

Abstract: Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.

Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.

Abstract: This application provides a method for the use of select quaternary ammonium antagonists to alpha-7 nAChR for the treatment of cancer and HIV and AIDS.

Abstract: Provided are methods of modulating, treating, reversing and/or preventing pain using tetrakis quaternary ammonium compounds, especially regarding pain of central and/or peripheral origin and/or pain which is nociceptive, neuropathic, somatic, visceral, and/or inflammatory in nature.

Abstract: N-n-Alkylation of nicotine converts nicotine from an agonist into an antagonist specifically for neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogs exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.

Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nociception and pain.

Abstract: Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.

Abstract: Provided are bis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.

Abstract: Provided are bis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.

Abstract: Provided are tetrakis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.

Abstract: Methods of delivering or administering stabilized formulations or compositions having predetermined ratios, or range of ratios, of constituent epimers to an individual or a mammal for treatment of central nervous system diseases, pathologies, and drug abuse and compositions for stabilizing the compositions. In one embodiment, the predetermined ratios of constituent epimers, or range of ratios, are predetermined ratios of 2-[6S-(2S-hydroxy-2-phenyl-ethyl)-1-methyl-piperidin-2R-yl]-1-phenyl-ethanone (2R-lobeline) and its epimer, 2-[6S-(2S-hydroxy-2-phenyl-ethyl)-1-methyl-piperidin-2S-yl]-1-phenyl-ethanone (2S-lobeline).

Abstract: N-n-Alkylation of nicotine converts nicotine from an agonist into an antagonist specifically for neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogs exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.

Abstract: Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: are used to treat diseases of the central nervous system, drug abuse and withdrawal therefrom as well as to treating eating disorders.

Abstract: Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: 1

Abstract: Pharmaceutical compounds comprising bridged nicotine analogs of N-octylnicotinium iodide (NONI) having selective antagonist properties at &agr;3&bgr;2-containing nicotinic receptor subtypes, and compositions containing these compounds. The compounds and compositions are used to treat central nervous system pathologies.

Abstract: Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: are used to treat diseases of the central nervous system, drug abuse and withdrawal therefrom as well as to treating eating disorders.

Abstract: Pharmaceutical compounds comprising bridged nicotine analogs of N-octylnicotinium iodide (NONI) having selective antagonist properties at &agr;3&bgr;2-containing nicotinic receptor subtypes, and compositions containing these compounds. The compounds and compositions are used to treat central nervous system pathologies.

Abstract: Lobeline and nicotine evoke [.sup.3 H]overflow from rat striatal slices preloaded with [.sup.3 H]dopamine ([.sup.3 H]DA). The lobeline-evoked overflow is calcium-independent and not antagonized by mecamylamine, suggesting a mechanism of action other than the stimulation of nicotinic receptors. Whereas nicotine stimulates nicotinic receptors, lobeline inhibits [.sup.3 H]DA uptake into synaptic vesicles and striatal synaptosomes. The results suggest that different mechanisms are responsible for the increase in striatal DA release evoked by lobeline and nicotine. [.sup.3 H]-Dihydrotetrabenazine [.sup.3 H]DTBZ), used routinely to probe a high-affinity binding site-on the vesicular monoamine transporter (VMAT2) binds to vesicle membranes from rat striatum. Lobeline inhibits [.sup.3 H]DTBZ binding with an IC.sub.50 of 0.90 .mu.M, consistent with its IC.sub.50 of 0.88 .mu.M for inhibition of [.sup.3 H]DA uptake into vesicles.