检测方案
≥98% (HPLC)
形式
solid
颜色
white
溶解性
H2O: >5 mg/mL
SMILES字符串
Cl.Cl.COc1ccccc1N2CCN(CC2)CCN3C(=O)CC4(CCCC4)CC3=O
InChI
1S/C22H31N3O3.2ClH/c1-28-19-7-3-2-6-18(19)24-13-10-23(11-14-24)12-15-25-20(26)16-22(17-21(25)27)8-4-5-9-22;;/h2-3,6-7H,4-5,8-17H2,1H3;2*1H
InChI key
NIBOMXUDFLRHRV-UHFFFAOYSA-N
基因信息
human ... ADRA1D(146) , HTR1A(3350)
生化/生理作用
BMY 7378 dihydrochloride is a partial 5-HT1A serotonin receptor agonist and selective α1D-adrenoceptor antagonist.
特点和优势
This compound is featured on the α1-Adrenoceptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
法律信息
Manufactured and sold with the permission of Bristol Myers Squibb Corporation.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
M Yang et al.
Naunyn-Schmiedeberg's archives of pharmacology, 355(4), 438-446 (1997-04-01)
We have used the alpha1D-adrenoceptor selective antagonist, BMY 7378, the alpha1D-selective agonists, adrenaline and phenylephrine, the alpha1A-selective antagonists, (+)-niguldipine, SB 216469 and WB4101, and the non-subtype-selective alpha1-adrenoceptor antagonist, nemonapride, to investigate the presence of alpha1D-adrenoceptors in rat tissues at the
M Eltze et al.
European journal of pharmacology, 378(1), 69-83 (1999-09-09)
The affinity for functional alpha1-adrenoceptor subtypes of buspirone in comparison with its close structural analogs and selective alpha1D-adrenoceptor antagonists, BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]dec ane-7,9-dione) and MDL 73005EF (8-[2-(1,4-benzodioxan-2-ylmethylamino)ethyl]-8-azaspiro+ ++[4.5]decane-7,9-dione), was determined, namely at subtype A in rat vas deferens and perfused
BMY 7378, a buspirone analog with high affinity, selectivity and low intrinsic activity at the 5-HT1A receptor in rat and guinea pig hippocampal membranes.
F D Yocca et al.
European journal of pharmacology, 137(2-3), 293-294 (1987-06-04)
M J Millan et al.
The Journal of pharmacology and experimental therapeutics, 268(1), 337-352 (1994-01-01)
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(indan-1-yl)ethyl]piperazine (S15931) competitively displaced the binding of [3H]-8-OH-DPAT at serotonin (5-HT)1A receptors with affinities (pKis) of 9.2, 8.8 and 8.9, respectively. These values compared favorably with those of the
T Sharp et al.
European journal of pharmacology, 176(3), 331-340 (1990-02-13)
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-2-(di-n-pro-pylamino)tetralin (8-OH-DPAT), BMY 7378 (0.25-5 mg/kg s.c.) did not
商品
Review alpha 1 adrenoceptors as well as their agonists, antagonists, and tissue expression patterns. We suggest several modulators and alternatives for working with a-1 adrenoreceptors.
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