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Merck
CN

B134

BMY 7378 dihydrochloride

≥98% (HPLC), solid

别名:

8-[2-[4-(2-Methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride

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关于此项目

经验公式（希尔记法）:
C22H31N3O3 · 2HCl
化学文摘社编号:
21102-95-4
分子量:
458.42
NACRES:
NA.77
PubChem Substance ID:
24278080
UNSPSC Code:
12352200
MDL number:
MFCD00153771

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产品名称

BMY 7378 dihydrochloride, ≥98% (HPLC), solid

InChI key

NIBOMXUDFLRHRV-UHFFFAOYSA-N

SMILES string

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

assay

≥98% (HPLC)

form

solid

color

white

solubility

H2O: >5 mg/mL

Gene Information

human ... ADRA1D(146), HTR1A(3350)

Biochem/physiol Actions

BMY 7378 dihydrochloride is a partial 5-HT1A serotonin receptor agonist and selective α1D-adrenoceptor antagonist.

Features and Benefits

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.

Legal Information

Manufactured and sold with the permission of Bristol Myers Squibb Corporation.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000214591
0000214591
0000100795
0000067919
0000012642

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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
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
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
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α1-Adrenoceptor Characteristics and Modulators

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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