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Nicotine Decreases Food Intake Through Activation of POMC Neurons
TLDR
It is demonstrated that nicotine decreases food intake and body weight by influencing the hypothalamic melanocortin system and identifies critical molecular and synaptic mechanisms involved in nicotine-induced decreases in appetite. Expand
5-Iodo-A-85380, an α4β2 Subtype-Selective Ligand for Nicotinic Acetylcholine Receptors
In an effort to develop selective radioligands for in vivo imaging of neuronal nicotinic acetylcholine receptors (nAChRs), we synthesized 5-iodo-3-(2(S)-azetidinylmethoxy)pyridine (5-iodo-A-85380)Expand
Cytisine-Based Nicotinic Partial Agonists as Novel Antidepressant Compounds
TLDR
Novel nicotinic partial agonists may provide new possibilities for development of drugs to treat mood disorders and animals showed dose-dependent antidepressant-like effects in all three behavioral paradigms. Expand
Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors.
TLDR
A series of pyridone ring-modified derivatives of (7R,9S)-(-)-cytisine evaluated for affinity and functional activity at neuromuscular alpha1beta1gammadelta, ganglionic alpha3beta4, and central neuronal alpha4beta2 subtypes of nicotinic receptors found that thiocytisine was relatively weak in potency and efficacy, but was significantly selective for the alpha4 beta2 subtype. Expand
5-Iodo-A-85380, an alpha4beta2 subtype-selective ligand for nicotinic acetylcholine receptors.
TLDR
The results of experiments characterizing this radioiodinated ligand in vitro suggest that this compound, labeled with (125)I or (123)I, is superior to other radioligands available for in vitro and in vivo studies of alpha4beta2 nAChRs, respectively. Expand
2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: synthesis, affinity for nicotinic acetylcholine receptors, and molecular modeling.
TLDR
The synthesis and in vitro nAChR binding of a series of 10 pyridine-modified analogues of A-85380, featuring a halogen substituent at position 2, 5, or 6 of the 3-pyridyl fragment are reported. Expand
Syntheses and evaluation of halogenated cytisine derivatives and of bioisosteric thiocytisine as potent and selective nAChR ligands.
TLDR
Three one-step syntheses of halogenated derivatives of (-)-cytisine featuring a halogen substituent at positions 3, 5 or 3 and 5 of the 2-pyridone fragment are developed, and the novel bioisosteric thiocytisine is prepared by oxygen-sulphur exchange. Expand
Smoking upregulates alpha4beta2* nicotinic acetylcholine receptors in the human brain.
TLDR
The up-regulation of alpha4beta2* nAChR upon chronic nicotine exposure via tobacco smoking incorporates subcortical brain regions which may play an important role in nicotine addiction. Expand
Syntheses and evaluation of pyridazine and pyrimidine containing bioisosteres of (+/-)-pyrido[3.4-b]homotropane and pyrido-[3.4-b]tropane as novel nAChR ligands.
TLDR
In comparison to PHT, well known to exhibit affinity for agonist binding sites in rat brain approximately equivalent to that of (+)-anatoxin-a, replacement of the pyridine by the bioisosteric pyridazine resulted in 30-fold lower affinity at the (alpha4)2(beta2)3 subtype. Expand
6-[18F]fluoro-A-85380, a novel radioligand for in vivo imaging of central nicotinic acetylcholine receptors.
TLDR
The novel radioligand, 6-[18F]FA, appears to be a suitable candidate for imaging nAChRs in human brain due to a target-to-non-target ratio of binding in primate brain similar to that previously determined for a labeled analog of epibatidine, [18F]. Expand
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