4-DAMPAn antagonist of mAChR M3

4-DAMP (CAS 1952-15-4)

4-DAMP | CAS 1952-15-4 is rated 5.0 out of 5 by 1.
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Application: An antagonist of mAChR M3
CAS Number: 1952-15-4
Purity: 98%
Molecular Weight: 451.4
Molecular Formula: C21H26INO2
* Refer to Certificate of Analysis for lot specific data (including water content).
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4-DAMP, or 4-diphenylacetoxy-N-methyl-piperidine methiodide, is an antagonist at muscarinic receptors. A deuterated [3H]4-DAMP derivative was demonstrated to bind mAChR M1 and mAChR M3 with high affinity, and mAChR M2 with low affinity. Blockade of mAChR M2 by 4-DAMP produced a dose-dependent reduction of blood pressure in spotaneously hypertensive rats. 4-DAMP is an inhibitor of mAChR M1, mAChR M2, mAChR M3, mAChR M4 and mAChR M5.


References

1. Barlow, R.B. and Shepherd, M.K. 1986. Br. J. Pharmacol. 89: 837-843. PMID: 3814912
2. Brezenoff, H.E., et al. 1988. Pharmacology. 36: 101-105. PMID: 3353437
3. Michel, A.D., et al. 1989. Eur. J. Pharmacol. 166: 459-466. PMID: 2806372

Physical State :
Solid
Solubility :
Soluble in warm water (3 mg/ml), DMSO (≥15 mg/ml), and methanol.
Storage :
Store at room temperature
Melting Point :
211-213° C
IC50 :
Muscarinic acetylcholine receptor M3: IC50 = 0.59 nM (human); Muscarinic acetylcholine receptor M4: IC50 = 1.1 nM (human); Muscarinic acetylcholine receptor M5: IC50 = 0.83 nM (human); Adenosine A3 receptor: IC50 = 1.9 nM (human)
Ki Data :
Muscarinic acetylcholine receptor M5: Ki= 0.42 nM (human); Muscarinic acetylcholine receptor M3: Ki= 0.42 nM (human); Muscarinic acetylcholine receptor M4: Ki= 0.66 nM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
3014059
MDL Number :
MFCD00078564
SMILES :
C[N+]1(CCC(CC1)OC(=O)C(C2=CC=CC=C2)C3=CC=CC=C3)C.[I-]

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Certificate of Analysis

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4-DAMP  Product Citations

See how others have used 4-DAMP. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 27576172  Liang, Z. et al. 2017. Neurourol. Urodyn. 36: 1261-1269.

PMID: # 25412212  Dai, Y. et al. 2015. Molecular medicine reports. 11: 2292-8.

PMID: # 23577721  Lu, X. et al. 2013. J. Cell. Mol. Med. 17: 664-71.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from Michel et al Michel et al. (PubMed ID 2806372) used 4-DAMP as ligand to selectively label muscarinic receptors of the rat submaxillary gland, heart, and cortex. -SCBT Publication Review
Date published: 2015-04-09
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