• ligands
  • Although nicotine (1a), a naturally occurring nAChR ligand, is associated with a variety of toxic side effects, there is no reason to believe that these side effects are inextricably linked to the beneficial effects of nicotinic ligands. (springer.com)
  • agonist
  • Thus, we and others have begun investigations to identify the structureactivity relationships (SAR) for nicotinic agonist and antagonist activity, and structure-affinity relationships (SAFIR) for central nAChR binding, to ultimately develop novel nicotinic agents with greater selectivity and reduced toxicity that may be useful for disorders involving nAChRs. (springer.com)
  • Changes in the response to a concomitantly administered adrenergic agonist or antagonist should be watched for when nicotine intake is altered during Nicotrol Inhaler therapy and/or smoking cessation (See PRECAUTIONS, Drug Interactions ). (drugs.com)
  • stimulant
  • Nicotine is a stimulant, so as well as creating a pleasurable feeling, it also raises your heart rate, improves your ability to pay attention and boosts memory . (ecigarettedirect.co.uk)
  • For smokers, this means that you inhale more deeply to get a more relaxing effect from nicotine and take shallower inhales to get more of a stimulant effect. (ecigarettedirect.co.uk)
  • inhalation
  • NICOTROL ® Inhaler (nicotine inhalation system) consists of a mouthpiece and a plastic cartridge delivering 4 mg of nicotine from a porous plug containing 10 mg nicotine. (drugs.com)
  • An intensive inhalation regimen (80 deep inhalations over 20 minutes) releases on the average 4 mg of the nicotine content of each cartridge of which about 2 mg is systemically absorbed. (drugs.com)
  • effects
  • One, the "inherent functionality model", assumes that primitive binding pockets are a necessary consequence of protein folding, and that the effects of small molecules on these (probably quite nonspecific) motifs has been honed by evolutionary pressures since then. (sciencemag.org)
  • I'm a medicinal chemist, someone who's used to seeing "magic methyl effects" where very small changes in ligand structure can make big differences in binding to a protein. (sciencemag.org)
  • Both smoking and nicotine can increase circulating cortisol and catecholamines, and tolerance does not develop to the catecholaminereleasing effects of nicotine. (drugs.com)
  • What Are The Short Term Effects of Nicotine On Your Body? (ecigarettedirect.co.uk)
  • When you vape or smoke, the short term effects of nicotine are the main thing you'll notice. (ecigarettedirect.co.uk)
  • subunit
  • Mutations indicate that a sequence (AGMI) at the end of the C terminus of the human α4 subunit forms a binding site required for 17β-estradiol potentiation. (jneurosci.org)
  • different
  • Even if those binding sites were completely different from one another , we'd be looking at a set of binding pockets in the thousands/tens of thousands range, most likely. (sciencemag.org)
  • activity
  • Barlow RB, Johnson O (1989) Relations between structure and nicotine-like activity: X-ray crystal structure analysis of (-)-cytisine and (-)-lobeline hydrochloride and a comparison with (-)-nicotine and other nicotine-like compounds. (springer.com)
  • Nonetheless, many members of this unplanned family showed real levels of binding to things like heme, and many even showed above-background levels of several types of enzymatic activity. (sciencemag.org)
  • form
  • This phosphorylation allows τ to bind together and form tangled threads [ 10 ]. (hindawi.com)
  • α-Cobratoxin can occur in both a monomeric form and a disulfide-bound dimeric form. (wikipedia.org)
  • As a homodimer it is still able to bind to muscle type and α7 nAChRs, but with a lower affinity than in its monomeric form. (wikipedia.org)
  • There are two forms of ChAT: Soluble form and membrane-bound form. (wikipedia.org)
  • The membrane-bound form of ChAT is associated with synaptic vesicles. (wikipedia.org)
  • similar
  • And that makes me think that I could probably take a set of binding pockets that Skolnick's people would call so similar as to be basically identical, and still find small molecules that would differentiate them. (sciencemag.org)
  • Neonicotinoids (sometimes shortened to neonics /ˈniːoʊnɪks/) are a class of neuro-active insecticides chemically similar to nicotine. (wikipedia.org)
  • single
  • The findings that β-estradiol requires the AGMI sequence but that a single C-terminal tryptophan is sufficient for potentiation by ethynyl β-estradiol indicate that the C terminus forms a binding site for these steroids. (jneurosci.org)
  • active
  • Of its two stereoisomers, S(-)nicotine is the more active. (drugs.com)
  • Choline is bound in the active site of ChAT by non-covalent interactions between the positively charged amine of choline and the hydroxyl group of Tyr552, in addition to a hydrogen bond between choline's hydroxyl group and a histidine residue, His324. (wikipedia.org)