4-DAMP
4-DAMP is a M3 cholinergic receptor antagonist, with a Kd value of 0.5 nM for the M3 cholinergic receptor expressed in the gastric smooth muscle cell. M3 cholinergic receptors are the predominant subtype of muscarinic acetylcholine receptors, which mediates the parasympathetic control of smooth muscle contraction and glandular secretion, muscarinic acetylcholine receptor agonist-induced increases in food intake and body weight, as well as the sympathetic cholinergic control of sweating. 4-DAMP is thought to be selective for M3 receptors in peripheral tissues, but only exhibits limited selectivity for muscarinic receptors in the central nervous system.?
References:
1.?Murthy KS, Makhlouf GM. Differential coupling of muscarinic m2 and m3 receptors to adenylyl cyclases V/VI in smooth muscle. Concurrent M2-mediated inhibition via Galphai3 and m3-mediated stimulation via Gbetagammaq. Journal of Biological Chemistry, 1997, 272(34): 21317-21324.
2.?Joan HB, Nora L. Chapter 15 - Acetylcholine and Muscarinic Receptors. Primer on the Autonomic Nervous System (Third Edition), 2012, 75-78.
3.?Collins D, Smith DA, Messer WS Jr. Regional binding of 4-diphenylacetoxy-N-methylpiperidine methobromide (4-DAMP) to muscarinic receptors in rat brain and comparative analysis of minimum energy conformations. Neurochemistry International, 1993, 22(3): 237-247.
4. Teixeira-Neto FJ, McDonell WN, Black WD, et al. Effects of muscarinic receptor antagonists on acetylcholine-induced contractions of jejunal smooth muscle in horses. Journal of Veterinary Pharmacology and Therapeutics, 2012, 35(4): 313-318.
| Physical Appearance | A solid |
| Storage | Store at RT |
| M.Wt | 451.33 |
| Cas No. | 1952-15-4 |
| Formula | C21H26INO2 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥17.45 mg/mL in DMSO |
| Chemical Name | 4-(2,2-diphenylacetoxy)-1,1-dimethylpiperidin-1-ium iodide |
| SDF | Download SDF |
| Canonical SMILES | O=C(C(C1=CC=CC=C1)C2=CC=CC=C2)OC3CC[N+](C)(C)CC3.[I-] |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[4] | |
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Cell lines |
Jejunal muscle strips of horses |
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Reaction Conditions |
10-8 ~ 10-6 M 4-DAMP for 30 min incubation |
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Applications |
4-DAMP effectively antagonized acetylcholine-induced contractions of jejunal smooth muscle in horses, with better performance than pirenzepine (a M1 cholinergic receptor antagonist) and methoctramine (a M2 cholinergic receptor antagonist). |
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Note |
The technical data provided above is for reference only. |
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References: 1. Murthy KS, Makhlouf GM. Differential coupling of muscarinic m2 and m3 receptors to adenylyl cyclases V/VI in smooth muscle. Concurrent M2-mediated inhibition via Galphai3 and m3-mediated stimulation via Gbetagammaq. Journal of Biological Chemistry, 1997, 272(34): 21317-21324. 2. Joan HB, Nora L. Chapter 15 - Acetylcholine and Muscarinic Receptors. Primer on the Autonomic Nervous System (Third Edition), 2012, 75-78. 3. Collins D, Smith DA, Messer WS Jr. Regional binding of 4-diphenylacetoxy-N-methylpiperidine methobromide (4-DAMP) to muscarinic receptors in rat brain and comparative analysis of minimum energy conformations. Neurochemistry International, 1993, 22(3): 237-247. 4. Teixeira-Neto FJ, McDonell WN, Black WD, et al. Effects of muscarinic receptor antagonists on acetylcholine-induced contractions of jejunal smooth muscle in horses. Journal of Veterinary Pharmacology and Therapeutics, 2012, 35(4): 313-318. |
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Quality Control & MSDS
- View current batch:
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
