2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Cell Cycle/DNA Damage Apoptosis Epigenetics
  3. mAChR Reactive Oxygen Species (ROS) DNA/RNA Synthesis Apoptosis SOD Sirtuin
  4. Arecaidine-propargyl ester

Arecaidine-propargyl ester is a selective M2 muscarinic receptor agonist with blood-brain barrier permeability, with a pKi of 5.91 for hm1, 7.06 for hm2, 6.07 for hm3, 6.01 for hm4, and 6.03 for hm5. Arecaidine-propargyl ester stimulates central and peripheral muscarinic receptors. Arecaidine-propargyl ester increases intracellular ROS, induces DNA damage and Apoptosis, and upregulates the expression of MnSOD and SIRT1. Arecaidine-propargyl ester reduces sympathetic nerve outflow, induces dose-dependent hypotension, and triggers negative chronotropic effects at high peripheral doses. Arecaidine-propargyl ester can be used in research related to Alzheimer's disease and glioblastoma.

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Arecaidine-propargyl ester

Arecaidine-propargyl ester Chemical Structure

CAS No. : 35516-99-5

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Arecaidine-propargyl ester Related Antibodies

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Description

Arecaidine-propargyl ester is a selective M2 muscarinic receptor agonist with blood-brain barrier permeability, with a pKi of 5.91 for hm1, 7.06 for hm2, 6.07 for hm3, 6.01 for hm4, and 6.03 for hm5. Arecaidine-propargyl ester stimulates central and peripheral muscarinic receptors. Arecaidine-propargyl ester increases intracellular ROS, induces DNA damage and Apoptosis, and upregulates the expression of MnSOD and SIRT1. Arecaidine-propargyl ester reduces sympathetic nerve outflow, induces dose-dependent hypotension, and triggers negative chronotropic effects at high peripheral doses. Arecaidine-propargyl ester can be used in research related to Alzheimer's disease and glioblastoma[1][2][3].

IC50 & Target[2][3]

mAChR1

5.91 (pKi)

mAChR2

7.06 (pKi)

mAChR3

6.07 (pKi)

mAChR4

6.01 (pKi)

mAChR5

6.03 (pKi)

SIRT1

 

In Vitro

Arecaidine-propargyl ester (0.01-1000 mM; 120 min) binds to cloned hm1, hm2, hm3, hm4, and hm5 muscarinic receptors expressed in CHO cells, with pKi values ranging from 5.91 to 7.06[2].
Arecaidine-propargyl ester (25-100 μM; 2 h) induces significant intracellular ROS production in glioblastoma cell lines U251MG and U87MG, and this effect is completely blocked by the ROS scavenger NAC[3].
Arecaidine-propargyl ester (100 μM; 72 h) induces significant apoptosis and reduces cell numbers in human glioblastoma cell lines U251MG and U87MG, with a stronger apoptotic effect on U251MG cells. Both of these effects are abrogated by the ROS scavenger NAC[3].
Arecaidine-propargyl ester (100 μM; 24-48 h) significantly upregulates the expression of SIRT1 protein in glioblastoma U251MG and U87MG cells in a time-dependent manner in vitro[3].
Arecaidine-propargyl ester (100 μM; 24-48 h) significantly upregulates the expression of MnSOD protein in U251MG and U87MG glioblastoma cells in a time-dependent manner[3].
Arecaidine-propargyl ester (100 μM; 24-48 h) significantly upregulates the mRNA expression level of Gadd45α in glioblastoma cell lines U251MG and U87MG[3].
Arecaidine-propargyl ester (100 μM; 24 h) increases total glutathione levels by 50% in U251MG glioblastoma cells, whereas no significant metabolic changes are detected in U87MG cells[3].
Arecaidine-propargyl ester (100 μM; 24-48 h) induces DNA double-strand breaks (detected by γ-H2AX positive rate) in glioblastoma cell lines U251MG and U87MG, and this effect depends on the activation of M2 muscarinic receptors in U251MG cells[3].
Arecaidine-propargyl ester (50-100 μM; 24 h) induces significant chromosomal aberrations in glioblastoma U251MG and U87MG cells; among them, U251MG cells exhibit higher sensitivity at 50 μM, and only U251MG cells show a significant increase in sister chromatid exchange levels at 50 μM[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Arecaidine-propargyl ester Related Antibodies

Apoptosis Analysis[3]

Cell Line: U251MG, U87MG human glioblastoma cell lines
Concentration: 100 μM
Incubation Time: 72 h
Result: Increased the apoptotic index in U87MG cells and U251MG cells.
Significantly reduced the apoptotic index in both cell lines, returning levels near control values when co-treated with 5 μM NAC.
Caused a significant decrease in cell number in both lines, an effect reversed by co-treatment with NAC.

RT-PCR[3]

Cell Line: U251MG, U87MG human glioblastoma cell lines
Concentration: 100 μM
Incubation Time: 24 h, 30 h, 48 h
Result: Caused a significant increase in Gadd45α mRNA expression in both cell lines.
Increased Gadd45α/18S ratios in U87MG cells.
Increased Gadd45α/18S ratios in U251MG cells.
In Vivo

Arecaidine-propargyl ester (left vertebral artery; femoral vein) exhibits potent central and peripheral hypotensive activity in anaesthetized cats, with an ED25 of 1.0 × 10-9 moles/kg via vertebral artery and 1.4 × 10-9 moles/kg via femoral vein, and does not alter heart rate with central administration[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: either sex, weight 2-4 kg (anaesthetized for cardiovascular function monitoring)[1]
Dosage: 1.0 × 10-9 moles/kg (vertebral artery); 1.4 × 10-9 moles/kg (femoral vein)
Administration: left vertebral artery; femoral vein
Result: Caused dose-dependent reduction in mean arterial pressure (intravenous), which was blocked by intravenous methylatropine (300 μg/kg) but not centrally administered atropine (30 μg/kg) or D-benzethimide (10 μg/kg).
Caused dose-dependent reduction in mean arterial pressure (vertebral artery), which was not blocked by intravenous methylatropine (300 μg/kg) but was blocked by vertebral artery-administered atropine (50 μg/kg) or D-benzethimide (10 μg/kg).
Did not alter heart rate with central administration; only relatively high intravenous doses caused a decrease in cardiac frequency.
Exhibited ED-25 of 1.0 × 10-9 moles/kg via vertebral artery and 1.4 × 10-9 moles/kg via femoral vein.
Molecular Weight

179.22

Formula

C10H13NO2
CAS No.
SMILES

O=C(C1=CCCN(C1)C)OCC#C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Arecaidine-propargyl ester Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Arecaidine-propargyl ester35516-99-5mAChRReactive Oxygen Species (ROS)DNA/RNA SynthesisApoptosisSODSirtuinMuscarinic acetylcholine receptorSuperoxide Dismutasemuscarinic receptorglioblastoma cellshm2U251MGU87MGhm4hm3blood-brain barrierhm1hm5Inhibitorinhibitorinhibit

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