| Name | DREADD agonist 21 |
| Description | DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM). |
| In vitro | DREADD agonist 21 is a highly selective and potent agonist for muscarinic DREADDs (pEC50 for hM1Dq=6.54 and that for hM4Di=7.77 in pERK assays)[2]. DREADD agonist 21 potently activates hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro (pEC50: 8.48±0.05) and it also potently activates hM1Dq, hM3Dq, and hM4Di. DREADD agonist 21 does not activate human M3 receptor (hM3). DREADD agonist 21 displays high binding affinities to 5HT2A and 5HT2C serotonin receptor, α1A adrenergic receptor, and H1 histamine receptor with Ki values of 66, 170, 280, and 6 nM, respectively[1]. In addition to being inactive at hM3, DREADD agonist 21, a potent full agonist of hM3Dq (EC50=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 binds to hM1, hM4, hM1Dq and hM4Di receptors (pKis of 5.97, 5.44, 7.20, and 6.75, respectively). |
| In vivo | DREADD agonist 21 has excellent pharmacokinetic properties, bioavailability and brain penetrability. DREADD agonist 21 (0.3, 1.0, and 3.0 mg/kg; i.p.) activates neuronal hM3Dq in mice. DREADD agonist 21 (0.1, 1, and 10 mg/kg; i.p.) shows 95.1% plasma protein binding and 95% brain protein bounding in mice[2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 75 mg/mL (269.44 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (7.19 mM), Sonication is recommended.
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| Keywords | α1A-adrenergic receptor | α1A adrenergic receptor | schizophrenia | receptors | neuronal | neurodegenerative | Muscarinic acetylcholine receptor | muscarinic | mAChR | M4 mAChR | M1 mAChR | Inhibitor | inhibit | hM4Di | hM4 | hM3Dq | hM1Dq | hM1 | HistamineReceptor | Histamine Receptor | H1 receptor | H1 histamine receptor | DREADD agonist-21 | DREADD agonist21 | DREADD agonist 21 | DREADD | disease | AdrenergicReceptor | Adrenergic Receptor | activation | acetylcholine | 5HTReceptor | 5HT2C serotonin receptor | 5-HT2C | 5HT2A serotonin receptor 5HT2A | 5-HT2A | 5HT Receptor |
| Inhibitors Related | Alverine citrate | Meclizine dihydrochloride | Urethane | Famotidine | 1,8-Cineole | Adenine | Sodium butanoate | Mitotane | N,N-Dicyclohexylcarbodiimide | Arecoline | Alginic acid | Cinchonidine |
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