| Description |
nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research[1].
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| Related Catalog |
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| In Vitro |
nAChR-IN-1 (100 nM) inhibits nAChR with inhibition rate of 90% in Xenovus oocytes, and suppresses AChR subtypes (mouse muscle-type (α1β1εδ) nAChR, three different pairwise combinations of rat neuronal alpha and beta subunits (α3β4, α4β2, and α3β2), and α7 homomeric neuronal nAChR) with IC50s (area) of 390, 1.2, 110, 75, 440, 460, 430, 2.7, 1.0, 1.4, and 18.3 nM, respectively, based on the decrease in the net charge of the ACh response[1].
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| In Vivo |
nAChR-IN-1 (20 mg/kg; s.c.; single dose) improves nicotine-induced hypomotility and hypothermia in a time-dependent manner in mice[1]. Animal Model: Nicotine-induced mice model[1] Dosage: 20 mg/kg Administration: Subcutaneous injection; single dose; 15 minutes prior to the injection of nicotine (1.5 mg/kg) Result: Increased locomotor activity in mice, even if nicotine-induced decrease. Showed no effect on body temperature. Animal Model: Tail-flick and hot-platemodel in mice[1] Dosage: 0, 0.1, 1, 5 mg/kg Administration: Subcutaneous injection; single dose Result: Blocked the antinociceptive effect of nicotine in the hot-plate. Time-dependently blocked nicotine-induced antinociception.
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| References |
[1]. Papke RL, et, al. Compositions et methodes d'inhibition selective des recepteurs nicotiniques de l'acetylcholine. WO2005032479A2
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