PNU 22394 hydrochloride5-HT2C agonist and 5-HT2A/2B partial agonist CAS# 15923-42-9 |
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Quality Control & MSDS
3D structure
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| Cas No. | 15923-42-9 | SDF | Download SDF |
| PubChem ID | 16759162 | Appearance | Powder |
| Formula | C13H17ClN2 | M.Wt | 236.74 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in water | ||
| Chemical Name | 6-methyl-2,3,4,5-tetrahydro-1H-azepino[4,5-b]indole;hydrochloride | ||
| SMILES | CN1C2=C(CCNCC2)C3=CC=CC=C31.Cl | ||
| Standard InChIKey | SAIGGEUWSYESTR-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C13H16N2.ClH/c1-15-12-5-3-2-4-10(12)11-6-8-14-9-7-13(11)15;/h2-5,14H,6-9H2,1H3;1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent 5-HT2C agonist and partial 5-HT2A/5-HT2B agonist. Non-selective between 5-HT2 receptor subtypes (Ki values are 18, 18 and 66 nM for human recombinant 5-HT2C, 5-HT2A and 5-HT2B receptors respectively). Reduces food intake in rats following subcutaneous administration and displays anorexigenic effects in humans. |
PNU 22394 hydrochloride Dilution Calculator
PNU 22394 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 4.224 mL | 21.1202 mL | 42.2404 mL | 84.4809 mL | 105.6011 mL |
| 5 mM | 0.8448 mL | 4.224 mL | 8.4481 mL | 16.8962 mL | 21.1202 mL |
| 10 mM | 0.4224 mL | 2.112 mL | 4.224 mL | 8.4481 mL | 10.5601 mL |
| 50 mM | 0.0845 mL | 0.4224 mL | 0.8448 mL | 1.6896 mL | 2.112 mL |
| 100 mM | 0.0422 mL | 0.2112 mL | 0.4224 mL | 0.8448 mL | 1.056 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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The selective alpha7 nicotinic acetylcholine receptor agonist PNU-282987 [N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide hydrochloride] enhances GABAergic synaptic activity in brain slices and restores auditory gating deficits in anesthetized rats.[Pubmed:15523001]
J Pharmacol Exp Ther. 2005 Mar;312(3):1213-22.
Schizophrenic patients are thought to have an impaired ability to process sensory information. This deficit leads to disrupted auditory gating measured electrophysiologically as a reduced suppression of the second of paired auditoryevoked responses (P50) and is proposed to be associated with decreased function and/or expression of the homomeric alpha7 nicotinic acetylcholine receptor (nAChR). Here, we provide evidence that N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide hydrochloride (PNU-282987), a novel selective agonist of the alpha7 nAChR, evoked whole-cell currents from cultured rat hippocampal neurons that were sensitive to the selective alpha7 nAChR antagonist methyllycaconitine (MLA) and enhanced GABAergic synaptic activity when applied to hippocampal slices. Amphetamine-induced sensory gating deficit, determined by auditory-evoked potentials in hippocampal CA3 region, was restored by systemic administration of PNU-282987 in chloral hydrate-anesthetized rats. Auditory gating of rat reticular thalamic neurons was also disrupted by amphetamine; however, PNU-282987 normalized gating deficit only in a subset of tested neurons (6 of 11). Furthermore, PNU-282987 improved the inherent hippocampal gating deficit occurring in a subpopulation of anesthetized rats, and enhanced amphetamine-induced hippocampal oscillation. We propose that the alpha7 nAChR agonist PNU-282987, via modulating/enhancing hippocampal GABAergic neurotransmission, improves auditory gating and enhances hippocampal oscillatory activity. These results provide further support for the concept that drugs that selectively activate alpha7 nAChRs may offer a novel, potential pharmacotherapy in treatment of schizophrenia.
