Abstract：
:We compared the anti-proliferative properties of 4-benzylphenoxy-N ethyl morpholine (morpho-BPE) and trifluopromazine (TFP) on both the human breast cancer cell lines, MCF7, and its tamoxifen-resistant variant RTx6. We found that the calmodulin antagonist trifluopromazine (TFP) which bound ABS weakly, inhibited MCF7 cell growth but did not follow the relationship observed for diphenylmethane derivatives between MCF7-inhibitory potencies and their Ki. Regarding the tamoxifen-resistant RTx6 cells, TFP but not morpho-BPE induced inhibition of the proliferation. Using a tritiated derivative of morpho-BPE, two distinct binding sites could be demonstrated. Indeed, a low affinity binding site was present in both cell lines whereas a high affinity binding site was mainly found in MCF7 cells although being in lower concentration (less than 10%) in RTx6 cells. Both tamoxifen and TFP displaced morpho-BPE from the two binding sites. The uptake and efflux of the tritiated drug were similar in the two cell lines. The drug did not appear to be metabolized. We concluded that TFP and morpho-BPE belong to distinct classes of molecules and that ABS mediates the anti-proliferative action of diphenylmethane derivatives but not the inhibitory effect of the calmodulin antagonist TFP.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Poirot M,Garnier M,Bayard F,Riviere I,Traore M,Wilson M,Fargin A,Faye JCdoi
10.1016/0006-2952(90)90539-wsubject
Has Abstractpub_date
1990-08-01 00:00:00pages
425-9issue
3eissn
0006-2952issn
1873-2968pii
0006-2952(90)90539-Wjournal_volume
40pub_type
杂志文章abstract：:HOE 731, a substituted thienoimidazole derivative, was studied on [14C] aminopyrine uptake and oxygen consumption in isolated rabbit gastric glands. HOE 731 caused a concentration-dependent inhibition of [14C]aminopyrine uptake during histamine and dbcAMP stimulation. The inhibition during dbcAMP stimulation was in ac...
journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(90)90360-w
更新日期：1990-10-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：2012-01-15 00:00:00
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pub_type： 杂志文章
doi：10.1016/0006-2952(82)90386-0
更新日期：1982-04-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：2000-05-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：1987-07-15 00:00:00
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pub_type： 杂志文章
doi：10.1016/0006-2952(94)90534-7
更新日期：1994-04-29 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2017.05.001
更新日期：2017-08-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(87)90380-7
更新日期：1987-01-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(84)90409-x
更新日期：1984-05-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(90)90108-w
更新日期：1990-06-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2014.10.016
更新日期：2015-01-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/s0006-2952(99)00186-0
更新日期：1999-09-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(92)90691-b
更新日期：1992-12-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(87)90060-8
更新日期：1987-05-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(89)90380-8
更新日期：1989-02-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(86)90762-8
更新日期：1986-12-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 临床试验,杂志文章
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更新日期：2020-08-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/s0006-2952(02)01419-3
更新日期：2002-11-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(89)90584-4
更新日期：1989-11-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(87)90363-7
更新日期：1987-02-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章,评审
doi：10.1016/0006-2952(87)90252-8
更新日期：1987-09-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章,评审
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更新日期：2017-11-15 00:00:00
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pub_type： 杂志文章
doi：10.1016/j.bcp.2017.11.016
更新日期：2018-02-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(94)90329-8
更新日期：1994-04-20 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(94)90044-2
更新日期：1994-08-17 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章,评审
doi：10.1016/0006-2952(95)02232-5
更新日期：1996-05-03 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2003.12.005
更新日期：2004-04-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/s0006-2952(01)00625-6
更新日期：2001-06-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2013.08.067
更新日期：2013-12-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2007.02.005
更新日期：2007-06-01 00:00:00
