MDL 72832 hydrochloride |
| カタログ番号GC10985 |
5-HT1A受容体のリガンド、強力かつ選択的
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 113777-40-5
Sample solution is provided at 25 µL, 10mM.
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MDL 72832 hydrochloride is a potent and selective ligand for 5-HT1A receptor with pIC50 value of 9.1 [1].
The 5-HT1A receptor is a G protein-coupled receptor for endogenous neurotransmitter serotonin (5-HT) and mediates inhibitory neurotransmission.
MDL 72832 hydrochloride is a potent and selective ligand for 5-HT1A receptor [1]. Also, MDL 72832 exhibited affinity with pKD values of 6.32 and 6.34 for 5-HT1C and 5-HT1D receptors, respectively [1].
In rats, MDL 72832 inhibited 8-OH-DPAT-induced cardiovascular effects. In guinea-pigs, 8-OH-DPAT inhibited the contraction of the field-stimulated guinea-pig ileum in a concentration-dependent way. While MDL 72832 inhibited 8-OH-DPAT-induced neuronal inhibition. MDL 72832 is a ligand for 5-HT1A receptor with mixed antagonist and agonist properties [1]. In pre-satiated rats, (+) -MDL 72832 (1.0 mg/kg) stimulated food intake and (-) -MDL 72832 (0.03 mg/kg) significantly increased food intake [2]. In rats, MDL 72832 increased postsynaptic 5-HT1A receptors mediating hypothermia and exhibited agonist property [3].
References:
[1]. Mir AK, Hibert M, Tricklebank MD, et al. MDL 72832: a potent and stereoselective ligand at central and peripheral 5-HT1A receptors. Eur J Pharmacol, 1988, 149(1-2): 107-120.
[2]. Neill JC, Cooper SJ. MDL 72832, a selective 5-HT1A receptor ligand, stereospecifically increases food intake. Eur J Pharmacol, 1988, 151(2): 329-332.
[3]. Millan MJ, Rivet JM, Canton H, et al. Induction of hypothermia as a model of 5-hydroxytryptamine1A receptor-mediated activity in the rat: a pharmacological characterization of the actions of novel agonists and antagonists. J Pharmacol Exp Ther, 1993, 264(3): 1364-1376.
| Cas No. | 113777-40-5 | SDF | |
| Chemical Name | 8-(4-(((2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methyl)amino)butyl)-8-azaspiro[4.5]decane-7,9-dione hydrochloride | ||
| Canonical SMILES | O=C(N1CCCCNCC2COC3=CC=CC=C3O2)CC4(CC1=O)CCCC4.Cl | ||
| Formula | C22H30N2O4.HCl | M.Wt | 422.95 |
| 溶解度 | Soluble to 5 mM in Water | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3643 mL | 11.8217 mL | 23.6435 mL |
| 5 mM | 0.4729 mL | 2.3643 mL | 4.7287 mL |
| 10 mM | 0.2364 mL | 1.1822 mL | 2.3643 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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