CAS 21102-95-4|BMY 7378 dihydrochloride
| Common Name | BMY 7378 dihydrochloride | ||
|---|---|---|---|
| CAS Number | 21102-95-4 | Molecular Weight | 458.422 |
| Density | / | Boiling Point | 585.6ºC at 760 mmHg |
| Molecular Formula | C22H33Cl2N3O3 | Melting Point | 196.5-198.5 °C |
| MSDS | ChineseUSA | Flash Point | 307.9ºC |
Names
| Name | 8-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-8-azaspiro[4.5]decane-7,9-dione,dihydrochloride |
|---|---|
| Synonym | More Synonyms |
BMY 7378 dihydrochloride BiologicalActivity
| Description | BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist[1][2]. |
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| Related Catalog | Research Areas >>Cardiovascular DiseaseSignaling Pathways >>GPCR/G Protein >>Adrenergic ReceptorSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor |
| Target | rat α1A-adrenergic receptor:800 nM (Ki) hamster alpha1B-adrenergic receptor:600 nM (Ki) rat alpha1D-adrenergic receptor:2 nM (Ki) 5-HT1A Receptor |
| In Vitro | BMY 7378 is selective for the alpha 1D-adrenoceptor subtype (pKi: hamster alpha 1b-adrenoceptor 6.2, human alpha 1b-adrenoceptor 7.2; bovine alpha 1c-adrenoceptor 6.1, human alpha 1c-adrenoceptor 6.6; rat alpha 1d-adrenoceptor 8.2, human alpha 1d-adrenoceptor 9.4) and has high affinity (pA2, 8.9) for rat aorta alpha 1-adrenoceptor[2]. |
| References | [1]. Piascik MT, et al. The specific contribution of the novel alpha-1D adrenoceptor to the contraction of vascular smooth muscle. J Pharmacol Exp Ther. 1995;275(3):1583-1589. [2]. Goetz AS, et al. BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors. Eur J Pharmacol. 1995;272(2-3):R5-R6. |
Chemical & Physical Properties
| Boiling Point | 585.6ºC at 760 mmHg |
|---|---|
| Melting Point | 196.5-198.5 °C |
| Molecular Formula | C22H33Cl2N3O3 |
| Molecular Weight | 458.422 |
| Flash Point | 307.9ºC |
| Exact Mass | 457.189911 |
| PSA | 53.09000 |
| LogP | 4.07140 |
| Appearance of Characters | solid | white |
| Vapour Pressure | 1.07E-13mmHg at 25°C |
| InChIKey | NIBOMXUDFLRHRV-UHFFFAOYSA-N |
| SMILES | COc1ccccc1N1CCN(CCN2C(=O)CC3(CCCC3)CC2=O)CC1.Cl.Cl |
| Storage condition | Store at RT |
| Water Solubility | H2O: soluble |
Toxicological Information
CHEMICAL IDENTIFICATION |
ACUTE TOXICITY DATA - TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 53600 ug/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 12,876,1969
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |
| RTECS | GY3996000 |
| HS Code | 2933599090 |
Customs
| HS Code | 2933599090 |
|---|---|
| Summary | 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
Articles6
More Articles| The Alpha-1D Is the Predominant Alpha-1-Adrenergic Receptor Subtype in Human Epicardial Coronary Arteries J. Am. Coll. Cardiol. 54 , 1137-45, (2009) Objectives The goal was to identify alpha-1-adrenergic receptor (AR) subtypes in human coronary arteries. | |
| Further investigation of the in vivo pharmacological properties of the putative 5-HT1A antagonist, BMY 7378. Eur. J. Pharmacol. 176 , 331, (1990) The present study examined the actions of the putative 5-HT1A antagonist BMY 7378 on central pre- and postsynaptic 5-HT1A function in the rat in vivo. Unlike the direct acting 5-HT1A agonist 8-hydroxy... | |
| Novel benzodioxopiperazines acting as antagonists at postsynaptic 5-HT1A receptors and as agonists at 5-HT1A autoreceptors: a comparative pharmacological characterization with proposed 5-HT1A antagonists. J. Pharmacol. Exp. Ther. 268 , 337-352, (1994) The novel benzodioxopiperazines [4-(benzodioxan-5-yl)1-[2- (benzocyclobutane-1-yl)ethyl]piperazine] (S 14489), [4-(benzodioxan-5-yl)1-(indan-2-yl)piperazine)] (S 15535) and [4-(benzodioxan-5-yl)1-[2(i... |
Synonyms
| BMY 7378 dihydrochloride |
| 8-Azaspiro[4.5]decane-7,9-dione, 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-, hydrochloride (1:2) |
| 8-{2-[4-(2-Methoxyphenyl)-1-piperazinyl]ethyl}-8-azaspiro[4.5]decane-7,9-dione dihydrochloride |
| MFCD00153771 |
| 8-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione dihydrochloride |
| 8-[2-[4-(2-Methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride |
