Pirenzepine Dihydrochloride CAS: 29868-97-1
MF: C19H21N5O2 2HCl
MW: 424.3
An mAChR M1 selective antagonist.

Pirenzepine Dihydrochloride (CAS 29868-97-1)

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アプリケーション: Pirenzepine Dihydrochloride is an mAChR M1 selective antagonist
CAS 番号: 29868-97-1
Purity: ≥99%
Molecular Weight: 424.3
Molecular Formula: C19H21N5O2 2HCl
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* Refer to Certificate of Analysis for lot specific data (including water content).
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Pirenzepine Dihydrochloride is an analogue of Pirenzepine. Pirenzepine is a selective antagonist for the mAChR M1 (M1 muscarinic receptor) and is reported to block presynaptic mAChR M1 as well as some reported inverse agonist activity. A study investigating the pharmacological characterization of the muscarinic receptors associated with ACh-induced pulmonary vasodilation in a rabbit model of pulmonary hypertension determined the IC50 to be 2.51x10-7M. Additional research studies have investigated the role of Pirenzepine in the pathophysiology of myopia. Other mAChR M1 antagonists offered include Telenzepine (sc-204332).


参考文献

1. Daeffler, L., et al. 1999. Br. J. Pharmacol. 126: 1246-1252. PMID: 10205015
2. Orii, R., et al. 2010. Biosci Trends. 4: 260-266. PMID: 21068480
3. Garcia, N., et al. 2010. J. Neurosci. 30: 16514-16522. PMID: 21147991
4. González, J.C., et al. 2011. Eur. J. Neurosci. 33: 69-81. PMID: 21091801

Physical State :
Solid
Solubility :
Soluble in water (50 mg/ml).
保存方法 :
Desiccate at room temperature
Melting Point :
192-198° C
Boiling Point :
541.7° C at 760 mmHg (Predicted)
IC50 :
Muscarinic acetylcholine receptor M1: IC50 = 3.8 nM (rat); mAChR M1: IC50 = 12 nM (human); Adenosine A3-R: IC50 = 22 nM (human); mAChR M4: IC50 = 246.8 nM (human); Muscarinic acetylcholine receptor M3: IC50 = 300 nM (rat)
Ki Data :
mAChR M1: Ki= 2.82 nM (human); Muscarinic acetylcholine receptor M1: Ki= 3.6 nM (bovine); Muscarinic acetylcholine receptor M1: Ki= 5.2 nM (rat); mAChR M4: Ki= 13.8 nM (human); Muscarinic acetylcholine receptor M3: Ki= 28 nM (rat); mAChR M5: Ki= 35.48 nM (human)
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
WGK Germany :
2
RTECS :
UU7883000
PubChem CID :
Merck Index :
14: 7491
MDL Number :
MFCD00055214
EC Number :
249-907-5
SMILES :
CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4.Cl.Cl

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Pirenzepine Dihydrochloride (CAS 29868-97-1)  参考文献

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引用 1 to 3 of 3 合計

PMID: # 34536573  Islam, MZ.|Kojima, S.|Sameshima, M.|Obi, T.|Yamazaki-Himeno, E.|Shiraishi, M.|Miyamoto, A.| et al. 2021. Comp Biochem Physiol C Toxicol Pharmacol. 109190.

PMID: # 24942113  Islam, MZ. et al. 2014. J. Vet. Med. Sci. 76: 1339-45.

PMID: # 22499874  Matsumoto, F. et al. 2012. Poult. Sci. 91: 1158-64.

引用 1 to 3 of 3 合計
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