-8-azaspiro[4.5]decane-7,9-dione dihydrochloride
8-(2-(4-(2-Methoxyphenyl)piperazin-1-yl)ethyl)-8-azaspiro[4.5]decane-7,9-dione dihydrochloride
CAS: 21102-95-4
Molecular Formula: C22H32ClN3O3
-8-azaspiro[4.5]decane-7,9-dione dihydrochloride - Names and Identifiers
-8-azaspiro[4.5]decane-7,9-dione dihydrochloride - Physico-chemical Properties
| Molecular Formula | C22H32ClN3O3 |
| Molar Mass | 421.97 |
| Solubility | H2O: soluble |
| Appearance | solid |
| Color | white |
| Storage Condition | Inert atmosphere,Room Temperature |
| Sensitive | IRRITANT |
| MDL | MFCD00153771 |
| In vitro study | BMY7378 is 10-fold more selective for α2c-adrenoceptors than other α2-adrenoceptors, with a pKi of 6.54. BMY 7378 selectively acts on the α1d-adrenoceptor subtype (PKi: hamster α1b-adrenoceptor 6.2, human α1b-adrenoceptor 7.2; Bovine α1c-adrenoceptor 6.1, human α1c-adrenoceptor 6.6; Rat α1d-adrenoceptor 8.2, human α1d-adrenoceptor 9.4). BMY 7378 produced dose-dependent inhibition in the dorsal raphe nucleus in rats at concentrations of 1 nM to 30 nM. |
| In vivo study | BMY 7378 (pA 2=8.67) was about 6.62 times more potent than yohimbine (pA 2=100) at norepinephrine-induced rat aortic constriction. BMY 7378 (pA 2, 6.48) antagonized the norepinephrine-induced contractile response in the human saphenous vein (α2c-adrenoceptor), which was 7.56 greater than that of yohimbine (pA 2,). 10 times lower. BMY 7378 dose-dependently (0.25-5 mg/kg s.c.) reduced the undetectable levels of forepaw pedaling and head shaking induced by 8-OH-DPAT (0.75 mg/kg s.c.) in rats. BMY 7378 dose-dependently significantly reduced 5-HT release in the ventral hippocampus of anesthetized rats as measured by microdialysis in vivo in rats. |
-8-azaspiro[4.5]decane-7,9-dione dihydrochloride - Risk and Safety
| WGK Germany | 3 |
| RTECS | GY3996000 |
-8-azaspiro[4.5]decane-7,9-dione dihydrochloride - Reference Information
| biological activity | BMY 7378 is a multi-target inhibitor that acts on α2C-adenoceptor and α1D-adenoceptor, pKi is 6.54 and 8.2 respectively, and is a mixed 5-HT1A receptor agonist and antagonist, pKi is 8.3. |
| target | TargetValue 5-HT1A 8.3(pIC50) α1D-adenoceptor 8.2(pKi) Dopamine D2 receptor 7.4(pIC50) α2C-adenoceptor () 6.54(pKi) 5-HT1C 6.4(pIC50) |
| Target | Value |
| 5-HT1A | 8.3(pIC50) |
| α1D-adenoceper | 8.2(pKi) |
| Dopamine D2 receptor | 7.4(pIC50) |
| α2C-adenoceper () | 6.54(pKi) |
| 5-HT1C | 6.4(pIC50) |
| in vitro study | the selectivity of BMY7378 to α2C-adrenoceptors is 10 times higher than that of other α2-adrenoceptors, and pKi is 6.54. BMY 7378 selectively acts on α 1D-adrenoceptor subtypes (PKi: hamster α 1b-adrenoceptor 6.2, human α 1b-adrenoceptor 7.2; Bovine α 1c-adrenoceptor 6.1, human α 1c-adrenoceptor 6.6; Rat α 1d-adrenoceptor 8.2, human α 1d-adrenoceptor 9.4). BMY 7378 produced a dose-dependent inhibition in the dorsal raphe nucleus in rats at concentrations of 1 nM to 30 nM. |
| in vivo study | BMY 7378 (pA 2 is 8.67) acts on norepinephrine-induced aortic contraction in rats, which is about 100 times more effective than yohimbine (pA 2 is 6.62). BMY 7378 (pA 2 is 6.48) has an antagonistic effect on norepinephrine-induced contractile response in human saphenous veins (α2C-adrenoceptor), which is 10 times lower than yohimbine (pA 2 is 7.56). BMY 7378 dose-dependently (0.25-5 mg/kg s.c.) decreased the unmeasured levels of forepaw pedaling and head shaking induced by 8-OH-DPAT (0.75 mg/kg s.c.) in rats. In the ventral hippocampus of anesthetized rats, BMY 7378 significantly reduced 5-HT release in a dose-dependent manner by microdialysis in rats. |
Last Update：2024-04-09 21:04:16
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