Selectivity of ABT-089 for α4β2* and α6β2* nicotinic acetylcholine receptors in brain

Activation of α4β2*/α6β2* nicotinic receptors alleviates anxiety during nicotine withdrawal without upregulating nicotinic receptors.

Although nicotine mediates its effects through several nicotinic acetylcholine receptor (nAChR) subtypes, it remains to be determined which nAChR subtypes directly mediate heightened anxiety during withdrawal. Relative success in abstinence has been found with the nAChR partial agonist varenicline (Chantix; Pfizer, Groton, CT); however, treatment with this drug fails to alleviate anxiety in ind...

Recent Developments in Novel Antidepressants Targeting α4β2-Nicotinic Acetylcholine Receptors

Nicotinic acetylcholine receptors (nAChRs) have been investigated for developing drugs that can potentially treat various central nervous system disorders. Considerable evidence supports the hypothesis that modulation of the cholinergic system through activation and/or desensitization/inactivation of nAChR holds promise for the development of new antidepressants. The introductory portion of thi...

JPET #211706 1 Activation of α4β2*/α6β2* Nicotinic Receptors Alleviates Anxiety During Nicotine Withdrawal Without Upregulating Nicotinic Receptors

Endogenous acetylcholine modulates impulsive action via α4β2 nicotinic acetylcholine receptors in rats

Title Endogenous acetylcholine modulates impulsive action via α4β2 nicotinic acetylcholine receptors in rats Author(s) Tsutsui-Kimura, Iku; Ohmura, Yu; Izumi, Takeshi; Yamaguchi, Taku; Yoshida, Takayuki; Yoshioka, Mitsuhiro Citation European Journal of Pharmacology, 641(2-3): 148-153 Issue Date 2010-09-01 DOI Doc URL http://hdl.handle.net/2115/43803 Right Type article (author version) Additiona...

Diverse strategies targeting α7 homomeric and α6β2* heteromeric nicotinic acetylcholine receptors for smoking cessation.

Preclinical studies suggest that a diversity of nicotinic acetylcholine receptors (nAChRs) with different sensitivities to nicotine may contribute to tobacco addiction. Using rodent intravenous nicotine self-administration as a preclinical model with good predictive validity for therapeutic efficacy for tobacco cessation, investigators have identified heteromeric α6β2* and homomeric α7 nAChRs a...