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MedKoo Cat#: 526847 | Name: PNU282987 HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PNU282987 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors. In animal studies, it shows nootropic effects, and derivatives may be useful in the treatment of schizophrenia, although PNU-282,987 is not suitable for use in humans because of excessive inhibition of the hERG antitarget.

Chemical Structure

PNU282987 HCl
PNU282987 HCl
CAS#123464-89-1 (HCl)

Theoretical Analysis

MedKoo Cat#: 526847

Name: PNU282987 HCl

CAS#: 123464-89-1 (HCl)

Chemical Formula: C14H18Cl2N2O

Exact Mass: 0.0000

Molecular Weight: 301.21

Elemental Analysis: C, 55.83; H, 6.02; Cl, 23.54; N, 9.30; O, 5.31

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,350.00 2 Weeks
500mg USD 2,850.00 2 Weeks
1g USD 3,850.00 2 Weeks
2g USD 6,450.00 2 Weeks
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Related CAS #
711085-63-1 (free base) 123464-89-1 (HCl)
Synonym
PNU282987; PNU-282987; PNU 282987; PNU282,987; PNU-282,987; PNU 282,987; PNU282987 HCl; PNU282987 hydrochloride
IUPAC/Chemical Name
N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chloro-benzamide monohydrochloride
InChi Key
HSEQUIRZHDYOIX-ZOWNYOTGSA-N
InChi Code
InChI=1S/C14H17ClN2O.ClH/c15-12-3-1-11(2-4-12)14(18)16-13-9-17-7-5-10(13)6-8-17;/h1-4,10,13H,5-9H2,(H,16,18);1H/t13-;/m0./s1
SMILES Code
O=C(N[C@H]1CN2CCC1CC2)C3=CC=C(Cl)C=C3.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# CAS#123464-89-1 (PNU282987 HCl) CAS#711085-63-1 (PNU282987 free base).
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM.
In vitro activity:
In the present study, using pharmacological inhibition and genetic knockout of α7nAChR, this study assessed the antiapoptotic effects of an α7nAChR agonist PNU-282987 in primary cultured astrocytes treated with 1-methyl-4-phenylpyridinium (MPP+). PNU-282987 promoted the viability of astrocytes, alleviated MPP+ induced apoptosis, and decreased the number of GFAP+/TUNEL+ cells. Meanwhile, PNU-282987 upregulated the expression of the antiapoptotic protein Bcl-2 and downregulated the expression of the apoptotic protein Bax and cleaved-caspase-3. Moreover, the suppression of the JNK-p53-caspase-3 signaling may underlie the neuroprotective property of PNU-282987. Therefore, PNU-282987 ameliorates astroglial apoptosis induced by MPP+ through α7nAChR-JNK-p53 signaling. Reference: Front Cell Neurosci. 2019 Nov 12;13:507. https://pubmed.ncbi.nlm.nih.gov/31780901/
In vivo activity:
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. This study proposes that the alpha7 nAChR agonist PNU-282987, via modulating/enhancing hippocampal GABAergic neurotransmission, improves auditory gating and enhances hippocampal oscillatory activity. Reference: J Pharmacol Exp Ther. 2005 Mar;312(3):1213-22. https://pubmed.ncbi.nlm.nih.gov/15523001/
Solvent mg/mL mM comments
Solubility
DMSO 10.0 33.20
Water 16.6 55.11
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 301.21 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Zhang Y, Ma R, Wang W, Deng Q, Cao C, Yu C, Li S, Shi L, Tian J. Activation of α7nAChR by PNU282987 improves cognitive impairment through inhibiting oxidative stress and neuroinflammation in D-galactose induced aging via regulating α7nAChR/Nrf2/HO-1 signaling pathway. Exp Gerontol. 2023 May;175:112139. doi: 10.1016/j.exger.2023.112139. Epub 2023 Mar 10. PMID: 36898594. 2. Hua Y, Yang B, Chen Q, Zhang J, Hu J, Fan Y. Activation of α7 Nicotinic Acetylcholine Receptor Protects Against 1-Methyl-4-Phenylpyridinium-Induced Astroglial Apoptosis. Front Cell Neurosci. 2019 Nov 12;13:507. doi: 10.3389/fncel.2019.00507. PMID: 31780901; PMCID: PMC6861188. 3. Spitsbergen JB, Webster SE, Linn CL. Functional Changes in the Adult Mouse Retina using an Alpha7 Nicotinic Acetylcholine Receptor Agonist after Blast Exposure. Neuroscience. 2023 Feb 21;512:1-15. doi: 10.1016/j.neuroscience.2022.12.017. Epub 2022 Dec 24. PMID: 36572172. 4. Hajós M, Hurst RS, Hoffmann WE, Krause M, Wall TM, Higdon NR, Groppi VE. 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. J Pharmacol Exp Ther. 2005 Mar;312(3):1213-22. doi: 10.1124/jpet.104.076968. Epub 2004 Nov 2. PMID: 15523001.
In vitro protocol:
1. Zhang Y, Ma R, Wang W, Deng Q, Cao C, Yu C, Li S, Shi L, Tian J. Activation of α7nAChR by PNU282987 improves cognitive impairment through inhibiting oxidative stress and neuroinflammation in D-galactose induced aging via regulating α7nAChR/Nrf2/HO-1 signaling pathway. Exp Gerontol. 2023 May;175:112139. doi: 10.1016/j.exger.2023.112139. Epub 2023 Mar 10. PMID: 36898594. 2. Hua Y, Yang B, Chen Q, Zhang J, Hu J, Fan Y. Activation of α7 Nicotinic Acetylcholine Receptor Protects Against 1-Methyl-4-Phenylpyridinium-Induced Astroglial Apoptosis. Front Cell Neurosci. 2019 Nov 12;13:507. doi: 10.3389/fncel.2019.00507. PMID: 31780901; PMCID: PMC6861188.
In vivo protocol:
1. Spitsbergen JB, Webster SE, Linn CL. Functional Changes in the Adult Mouse Retina using an Alpha7 Nicotinic Acetylcholine Receptor Agonist after Blast Exposure. Neuroscience. 2023 Feb 21;512:1-15. doi: 10.1016/j.neuroscience.2022.12.017. Epub 2022 Dec 24. PMID: 36572172. 2. Hajós M, Hurst RS, Hoffmann WE, Krause M, Wall TM, Higdon NR, Groppi VE. 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. J Pharmacol Exp Ther. 2005 Mar;312(3):1213-22. doi: 10.1124/jpet.104.076968. Epub 2004 Nov 2. PMID: 15523001.
1: Honwad HH, Najibi M, Koscso B, Bogunovic M, Irazoqui JE. TFEB-Mediated Pro- inflammatory Response in Murine Macrophages Induced by Acute Alpha7 Nicotinic Receptor Activation. bioRxiv [Preprint]. 2024 Aug 10:2024.01.26.577408. doi: 10.1101/2024.01.26.577408. PMID: 39211236; PMCID: PMC11361017. 2: Xu FF, Li ZC, Zhang WJ, Li Q, Li DJ, Meng HB, Shen FM, Fu H. Activation of α7 nicotinic acetylcholine receptors inhibits hepatic necroptosis and ameliorates acute liver injury in mice. Anesthesiology. 2024 Aug 26. doi: 10.1097/ALN.0000000000005206. Epub ahead of print. PMID: 39186677. 3: AlSharari SD, Alameen AA, Aldafiri FS, Ali YS, Alshammari MA, Sari Y, Damaj MI. Activation of α7 nicotinic receptors attenuated hyperalgesia and anxiety induced by palatable obesogenic diet withdrawal. J Pharmacol Sci. 2024 Oct;156(2):86-101. doi: 10.1016/j.jphs.2024.07.006. Epub 2024 Jul 22. PMID: 39179339. 4: Wu HR, Zhang CN, Dou BQ, Chen NY, Gao DF, Zou PS, Pan CX, Gu JH, Mo DL, Su JC. Identification of O-arylated huperzinines as novel cholinergic anti- inflammatory pathway agonists against gout arthritis. Bioorg Chem. 2024 Nov;152:107716. doi: 10.1016/j.bioorg.2024.107716. Epub 2024 Aug 21. PMID: 39178707. 5: Lykhmus O, Tzeng WY, Koval L, Uspenska K, Zirdum E, Kalashnyk O, Garaschuk O, Skok M. Impairment of brain function in a mouse model of Alzheimer's disease during the pre-depositing phase: The role of α7 nicotinic acetylcholine receptors. Biomed Pharmacother. 2024 Sep;178:117255. doi: 10.1016/j.biopha.2024.117255. Epub 2024 Aug 7. PMID: 39116785. 6: Alameen AA, AlSharari SD, Alshammari MA, Damaj MI, Sari Y. The potential effect of α7 nicotinic receptors modulation on palatable food-induced dependence-like behaviors. Saudi Pharm J. 2024 Aug;32(8):102138. doi: 10.1016/j.jsps.2024.102138. Epub 2024 Jul 4. PMID: 39109164; PMCID: PMC11301368. 7: Görgülü I, Jagannath V, Pons S, Koniuszewski F, Groszer M, Maskos U, Huck S, Scholze P. The human-specific nicotinic receptor subunit CHRFAM7A reduces α7 receptor function in human induced pluripotent stem cells-derived and transgenic mouse neurons. Eur J Neurosci. 2024 Sep;60(5):4893-4906. doi: 10.1111/ejn.16474. Epub 2024 Jul 28. PMID: 39073048. 8: Chen F, Zhang Z, Zhang H, Guo P, Feng J, Shen H, Liu X. Activation of α7 Nicotinic Acetylcholine Receptor Improves Muscle Endurance by Upregulating Orosomucoid Expression and Glycogen Content in Mice. J Cell Biochem. 2024 Jul 16:e30630. doi: 10.1002/jcb.30630. Epub ahead of print. PMID: 39014907. 9: Vanzo-Sparks HK, Webster SE, Webster MK, Linn CL. Quantification of Proliferating and Mitotically Active Retinal Cells in Mice by Flow Cytometry. Bio Protoc. 2024 Jul 5;14(13):e5024. doi: 10.21769/BioProtoc.5024. PMID: 39011369; PMCID: PMC11247376. 10: Shen L, Zhong X, Ji H, Yang S, Jin J, Lyu C, Ren Y, Xiao Y, Zhang Y, Fang S, Lin N, Tou J, Shu Q, Lai D. Macrophage α7nAChR alleviates the inflammation of neonatal necrotizing enterocolitis through mTOR/NLRP3/IL-1β pathway. Int Immunopharmacol. 2024 Sep 30;139:112590. doi: 10.1016/j.intimp.2024.112590. Epub 2024 Jul 13. PMID: 38996778. 11: Linn DM. Target identification and validation of the alpha7 nicotinic acetylcholine receptor as a potential therapeutic target in retinal disease. Front Ophthalmol (Lausanne). 2023 Jul 24;3:1190439. doi: 10.3389/fopht.2023.1190439. PMID: 38983049; PMCID: PMC11182235. 12: Wu L, Li J, Zou J, Tang D, Chen R. Vagus nerve modulates acute-on-chronic liver failure progression via CXCL9. Chin Med J (Engl). 2024 Jun 28. doi: 10.1097/CM9.0000000000003104. Epub ahead of print. PMID: 38945689. 13: Chen SH, Damborsky JC, Wilson BC, Fannin RD, Ward JM, Gerrish KE, He B, Martin NP, Yakel JL. α7 nicotinic receptor activation mitigates herpes simplex virus type 1 infection in microglia cells. Antiviral Res. 2024 Aug;228:105934. doi: 10.1016/j.antiviral.2024.105934. Epub 2024 Jun 15. PMID: 38880195; PMCID: PMC11250235. 14: Jin Z, Shen Z, Yan S, Chen G, Yin Y, Zhang Y, Wu X. Electroacupuncture ameliorates gastrointestinal dysfunction by modulating DMV cholinergic efferent signals to drive the vagus nerve in p-MCAO rats. Heliyon. 2024 Apr 9;10(8):e29426. doi: 10.1016/j.heliyon.2024.e29426. PMID: 38638995; PMCID: PMC11024612. 15: Ongnok B, Prathumsap N, Chunchai T, Pantiya P, Arunsak B, Chattipakorn N, Chattipakorn SC. Nicotinic and Muscarinic Acetylcholine Receptor Agonists Counteract Cognitive Impairment in a Rat Model of Doxorubicin-Induced Chemobrain via Attenuation of Multiple Programmed Cell Death Pathways. Mol Neurobiol. 2024 Apr 3. doi: 10.1007/s12035-024-04145-0. Epub ahead of print. PMID: 38568417. 16: Kalashnyk O, Lykhmus O, Sullivan R, Komisarenko S, Skok M. Agonists or positive allosteric modulators of α7 nicotinic acetylcholine receptor prevent interaction of SARS-Cov-2 receptor-binding domain with astrocytoma cells. Biochem Biophys Res Commun. 2024 May 21;709:149825. doi: 10.1016/j.bbrc.2024.149825. Epub 2024 Mar 25. PMID: 38537599. 17: Xia XM, Duan Y, Wang YP, Han RX, Dong YF, Jiang SY, Zheng Y, Qiao C, Cao L, Lu X, Lu M. Vagus nerve stimulation as a promising neuroprotection for ischemic stroke via α7nAchR-dependent inactivation of microglial NLRP3 inflammasome. Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365. doi: 10.1038/s41401-024-01245-4. Epub 2024 Mar 19. PMID: 38504011; PMCID: PMC11192746. 18: Zhou Z, Yang Y, Wei Y, Xie Y. Remimazolam Attenuates LPS-Derived Cognitive Dysfunction via Subdiaphragmatic Vagus Nerve Target α7nAChR-Mediated Nrf2/HO-1 Signal Pathway. Neurochem Res. 2024 May;49(5):1306-1321. doi: 10.1007/s11064-024-04115-x. Epub 2024 Mar 12. PMID: 38472553; PMCID: PMC10991060. 19: Zhang X, Wang H, Cai X, Zhang A, Liu E, Li Z, Jiang T, Li D, Ding W. α7nAChR Activation Combined with Endothelial Progenitor Cell Transplantation Attenuates Lung Injury in Diabetic Rats with Sepsis through the NF-κB Pathway. Inflammation. 2024 Aug;47(4):1344-1355. doi: 10.1007/s10753-024-01980-0. Epub 2024 Feb 1. PMID: 38302679. 20: Tsotsokou G, Kouri V, Papatheodoropoulos C. α7 nicotinic acetylcholine receptors induce long-term synaptic enhancement in the dorsal but not ventral hippocampus. Synapse. 2024 Jan;78(1):e22285. doi: 10.1002/syn.22285. PMID: 38287475.