Pirenzepine dihydrochloride

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Cat.No. 1071 - Pirenzepine dihydrochloride | C19H21N5O2.2HCl | CAS No. 29868-97-1
Description: Selective M1 muscarinic antagonist
Chemical Name: 5,11-Dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (10)
Literature

Biological Activity

M1 muscarinic receptor selective antagonist. Inverse agonist activity reported.

Technical Data

M. Wt 424.33
Formula C19H21N5O2.2HCl
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 29868-97-1
PubChem ID 71405
InChI Key FFNMBRCFFADNAO-UHFFFAOYSA-N
Smiles O=C1C3=C(C=CC=C3)N(C(CN4CCN(CC4)C)=O)C2=C(C=CC=N2)N1.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 100 mM in water

Preparing Stock Solutions

The following data is based on the product molecular weight 424.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.36 mL 11.78 mL 23.57 mL
5 mM 0.47 mL 2.36 mL 4.71 mL
10 mM 0.24 mL 1.18 mL 2.36 mL
50 mM 0.05 mL 0.24 mL 0.47 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Daeffler et al (1999) Inverse agonist activity of pirenzepine at M2 muscarinic acetylcholine receptors. Br.J.Pharmacol. 126 1246 PMID: 10205015

Doods et al (1994) Pharmacological profile of selective muscarinic receptor antagonists on guinea-pig ileal smooth muscle. Eur.J.Pharmacol. 253 275 PMID: 8200421

Eglen et al (1996) Muscarinic receptor subtypes and smooth muscle function. Pharmacol.Rev. 48 531 PMID: 8981565

Hammer et al (1980) Pirenzepine distinguishes between different subclasses of muscarinic receptors. Nature 283 90 PMID: 7350532


If you know of a relevant reference for Pirenzepine dihydrochloride, please let us know.

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Keywords: Selective M1 muscarinic antagonists Receptors Acetylcholine ACh M1 Receptors

10 Citations for Pirenzepine dihydrochloride

Citations are publications that use Tocris products. Selected citations for Pirenzepine dihydrochloride include:

Nadal et al (2016) Presynaptic muscarinic acetylcholine autoreceptors (M1, M2 and M4 subtypes), adenosine receptors (A1 and A2A) and tropomyosin-related kinase B receptor (TrkB) modulate the developmental synapse elimination process at the neuromuscular junction. Front Cell Neurosci 9 67 PMID: 27339059

Ahmed (2016) Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models. Physiological Reports 4  e13069 PMID: 28039410

Pediani et al (2016) Dynamic regulation of quaternary organization of the M1 muscarinic receptor by subtype-selective antagonist drugs. J.Biol.Chem. 291 13132 PMID: 27080256

Tian et al (2016) STEP activation by Gαq coupled GPCRs opposes Src regulation of NMDA receptors containing the GluN2A subunit Scientific Reports 6 36684  PMID: 27857196

Tozzi et al (2015) Endogenous 17β-estradiol is required for activity-dependent long-term potentiation in the striatum: interaction with the dopaminergic system. Front Cell Neurosci 9 192 PMID: 26074768

Martin et al (2015) Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex. Proc Natl Acad Sci U S A 9 457 PMID: 26648844

Pacini et al (2014) M2muscarinic receptors inhibit cell proliferation and migration in urothelial bladder cancer cells. Cancer Biol Ther 15 1489 PMID: 25482946

Mans et al (2014) An acetylcholinesterase inhibitor, eserine, induces long-term depression at CA3-CA1 synapses in the hippocampus of adult rats. J Neurophysiol 112 2388 PMID: 25143547

Tozzi et al (2012) A2A adenosine receptor antagonism enhances synaptic and motor effects of cocaine via CB1 cannabinoid receptor activation. PLoS One 7 e38312 PMID: 22715379

Buchanan et al (2010) Facilitation of long-term potentiation by muscarinic M(1) receptors is mediated by inhibition of SK channels. Neuron 68 948 PMID: 21145007


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