DREADD Agonist 21
DREADD agonist 21
CAS: 56296-18-5
Molecular Formula: C17H18N4
DREADD Agonist 21 - Names and Identifiers
DREADD Agonist 21 - Physico-chemical Properties
| Molecular Formula | C17H18N4 |
| Molar Mass | 278.35 |
| Density | 1.28±0.1 g/cm3(Predicted) |
| Boling Point | 470.1±55.0 °C(Predicted) |
| Solubility | DMSO: ≥ 78 mg/mL |
| pKa | 8.56±0.10(Predicted) |
| Storage Condition | -20℃ |
| Use | DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptor (hM3Dq) agonist (EC50=1.7 nM). |
| In vitro study | DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC 50 =1.7 nM) and does not activate human M3 receptor (hM3). In addition to being inactive at hM3, DREADD agonist 21, a potent full agonist of hM3Dq (EC 50 =1.7 nM), is only 3.5-fold selective for hM3Dq over H1, 40-fold selective over 5HT2A, 100-fold selective over 5HT2C, and 165-fold selective over α1A. DREADD agonist 21 shows high binding affinities to 5HT2A and 5HT2C serotonin receptor, α1A adrenergic receptor, and H1 histamine receptor with K i values of 66, 170, 280, and 6 nM, respectively. DREADD agonist 21 potently activates hM1Dq, hM3Dq, and hM4Di. DREADD agonist 21 binds to hM1, hM4, hM1Dq and hM4Di receptors with pK i s of 5.97, 5.44, 7.20, and 6.75, respectively. DREADD agonist 21 potently activates hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro with a pEC 50 of 8.48±0.05. DREADD agonist 21 is a highly selective and potent agonist for muscarinic DREADDs (pEC 50 for hM1Dq=6.54 and that for hM4Di=7.77 in pERK assays). |
| In vivo study | DREADD agonist 21 (0.3, 1.0, and 3.0 mg/kg; i.p.) activates neuronal hM3Dq in mice. DREADD agonist 21 has excellent bioavailability, pharmacokinetic properties, and brain penetrability. DREADD agonist 21 (0.1, 1, and 10 mg/kg; i.p.) displays 95.1% plasma protein binding and 95% brain protein bounding in mice. |
DREADD Agonist 21 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.593 ml | 17.963 ml | 35.926 ml |
| 5 mM | 0.719 ml | 3.593 ml | 7.185 ml |
| 10 mM | 0.359 ml | 1.796 ml | 3.593 ml |
| 5 mM | 0.072 ml | 0.359 ml | 0.719 ml |
Last Update：2024-01-02 23:10:35
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