Matches in SemOpenAlex for { <https://semopenalex.org/work/W2107979307> ?p ?o ?g. }
- W2107979307 endingPage "551" @default.
- W2107979307 startingPage "513" @default.
- W2107979307 abstract "Despite the proven efficacy of current pharmacotherapies for tobacco dependence, relapse rates continue to be high, indicating that novel medications are needed. Currently, several smoking cessation agents are available, including varenicline (Chantix®), bupropion (Zyban®), and cytisine (Tabex®). Varenicline and cytisine are partial agonists at the α4β2* nicotinic acetylcholine receptor (nAChR). Bupropion is an antidepressant but is also an antagonist at α3β2* ganglionic nAChRs. The rewarding effects of nicotine are mediated, in part, by nicotine-evoked dopamine (DA) release leading to sensitization, which is associated with repeated nicotine administration and nicotine addiction. Receptor antagonists that selectivity target central nAChR subtypes mediating nicotine-evoked DA release should have efficacy as tobacco use cessation agents with the therapeutic advantage of a limited side-effect profile. While α-conotoxin MII (α-CtxMII)-insensitive nAChRs (e.g., α4β2*) contribute to nicotine-evoked DA release, these nAChRs are widely distributed in the brain, and inhibition of these receptors may lead to nonselective and untoward effects. In contrast, α-CtxMII-sensitive nAChRs mediating nicotine-evoked DA release offer an advantage as targets for smoking cessation, due to their more restricted localization primarily to dopaminergic neurons. Small drug-like molecules that are selective antagonists at α-CtxMII-sensitive nAChR subtypes that contain α6 and β2 subunits have now been identified. Early research identified a variety of quaternary ammonium analogs that were potent and selective antagonists at nAChRs mediating nicotine-evoked DA release. More recent data have shown that novel, nonquaternary bis-1,2,5,6-tetrahydropyridine analogs potently inhibit (IC50<1nM) nicotine-evoked DA release in vitro by acting as antagonists at α-CtxMII-sensitive nAChR subtypes; these compounds also decrease NIC self-administration in rats." @default.
- W2107979307 created "2016-06-24" @default.
- W2107979307 creator A5009450662 @default.
- W2107979307 creator A5030875271 @default.
- W2107979307 creator A5083049265 @default.
- W2107979307 date "2014-01-01" @default.
- W2107979307 modified "2023-09-26" @default.
- W2107979307 title "Nicotinic Receptor Antagonists as Treatments for Nicotine Abuse" @default.
- W2107979307 cites W1515685619 @default.
- W2107979307 cites W1531561158 @default.
- W2107979307 cites W1560891849 @default.
- W2107979307 cites W1568881365 @default.
- W2107979307 cites W1721085211 @default.
- W2107979307 cites W1818352744 @default.
- W2107979307 cites W1963825419 @default.
- W2107979307 cites W1965034508 @default.
- W2107979307 cites W1965657664 @default.
- W2107979307 cites W1966092923 @default.
- W2107979307 cites W1966331187 @default.
- W2107979307 cites W1966683160 @default.
- W2107979307 cites W1968189433 @default.
- W2107979307 cites W1969169809 @default.
- W2107979307 cites W1970133822 @default.
- W2107979307 cites W1974426776 @default.
- W2107979307 cites W1978262730 @default.
- W2107979307 cites W1982378333 @default.
- W2107979307 cites W1982415425 @default.
- W2107979307 cites W1986445622 @default.
- W2107979307 cites W1988168385 @default.
- W2107979307 cites W1989689679 @default.
- W2107979307 cites W1993112595 @default.
- W2107979307 cites W2000935469 @default.
- W2107979307 cites W2002357983 @default.
- W2107979307 cites W2003949112 @default.
- W2107979307 cites W2004164502 @default.
- W2107979307 cites W2006969332 @default.
- W2107979307 cites W2008579253 @default.
- W2107979307 cites W2010309382 @default.
- W2107979307 cites W2011246896 @default.
- W2107979307 cites W2012120634 @default.
- W2107979307 cites W2015693259 @default.
- W2107979307 cites W2016015627 @default.
- W2107979307 cites W2019952241 @default.
- W2107979307 cites W2023051622 @default.
- W2107979307 cites W2025102684 @default.
- W2107979307 cites W2031417710 @default.
- W2107979307 cites W2034677985 @default.
- W2107979307 cites W2035016952 @default.
- W2107979307 cites W2038195629 @default.
- W2107979307 cites W2038601983 @default.
- W2107979307 cites W2043019023 @default.
- W2107979307 cites W2045851061 @default.
- W2107979307 cites W2046343373 @default.
- W2107979307 cites W2048118897 @default.
- W2107979307 cites W2049996304 @default.
- W2107979307 cites W2051648601 @default.
- W2107979307 cites W2054228421 @default.
- W2107979307 cites W2058079526 @default.
- W2107979307 cites W2058496420 @default.
- W2107979307 cites W2058697975 @default.
- W2107979307 cites W2058867245 @default.
- W2107979307 cites W2060286371 @default.
- W2107979307 cites W2063032208 @default.
- W2107979307 cites W2065671645 @default.
- W2107979307 cites W2072842977 @default.
- W2107979307 cites W2076338351 @default.
- W2107979307 cites W2078076047 @default.
- W2107979307 cites W2078579469 @default.
- W2107979307 cites W2081135796 @default.
- W2107979307 cites W2081470885 @default.
- W2107979307 cites W2081808154 @default.
- W2107979307 cites W2081870289 @default.
- W2107979307 cites W2084304884 @default.
- W2107979307 cites W2087568785 @default.
- W2107979307 cites W2088956467 @default.
- W2107979307 cites W2090082728 @default.
- W2107979307 cites W2092519884 @default.
- W2107979307 cites W2095392419 @default.
- W2107979307 cites W2097322630 @default.
- W2107979307 cites W2104748850 @default.
- W2107979307 cites W2106245886 @default.
- W2107979307 cites W2110027375 @default.
- W2107979307 cites W2115872169 @default.
- W2107979307 cites W2116846032 @default.
- W2107979307 cites W2117452133 @default.
- W2107979307 cites W2118190133 @default.
- W2107979307 cites W2120593159 @default.
- W2107979307 cites W2121492367 @default.
- W2107979307 cites W2127193609 @default.
- W2107979307 cites W2130326884 @default.
- W2107979307 cites W2131349644 @default.
- W2107979307 cites W2133701994 @default.
- W2107979307 cites W2133971381 @default.
- W2107979307 cites W2134235644 @default.
- W2107979307 cites W2135015777 @default.
- W2107979307 cites W2137599927 @default.
- W2107979307 cites W2140230791 @default.
- W2107979307 cites W2140401786 @default.