Abstract:
:Two novel 8 alpha-amino ergolines (CH 29-717 and CU 32-085) have been shown to inhibit secretion of prolactin in rats in vivo. However, when tested for dopaminomimetic potency on pituitary cell culture preparations in vitro, CH 29-717 inhibited prolactin release with an IC50 = 4 X 10(-9) M. In the same model the 1-methyl-derivative CU 32-085 was only weakly active even at high concentrations. When both compounds were incubated together, CU 32-085 displayed an inhibitory effect on the prolactin release restriction caused by CH 29-717. The activities were not time-dependent since similar results were obtained with incubation for 3 or 24 h. These results support the hypothesis that the 1-methyl ergoline derivative CU 32-085 is a partial agonist and becomes fully active in vivo only after metabolic conversion.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Markó Mdoi
10.1016/0014-2999(84)90167-5subject
Has Abstractpub_date
1984-06-01 00:00:00pages
263-6issue
3-4eissn
0014-2999issn
1879-0712pii
0014-2999(84)90167-5journal_volume
101pub_type
杂志文章abstract::The interaction between endogenous nitric oxide (NO), elicited by administration of Escherichia coli lipopolysaccharide, and cyclooxygenase system, in ethanol-induced injury in rat gastric mucosa, was investigated. Administration of graded doses of lipopolysaccharide reduced the gastric mucosal injury in response to e...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00161-7
更新日期:1998-05-08 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(00)00930-4
更新日期:2001-01-12 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(80)90281-2
更新日期:1980-03-21 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90213-6
更新日期:1989-04-25 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(03)01866-1
更新日期:2003-06-27 00:00:00
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journal_title:European journal of pharmacology
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doi:10.1016/s0014-2999(99)00928-0
更新日期:2000-03-03 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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更新日期:2003-02-21 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01501-x
更新日期:1998-01-12 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(83)90140-1
更新日期:1983-09-30 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.05.015
更新日期:2006-07-17 00:00:00
abstract::The excitatory mechanism of central sympathetic outflow induced by interleukin-1 beta was investigated in urethane-anesthetized rats. Intracerebroventricular administration of interleukin-1 beta induced a gradually developing elevation of plasma noradrenaline levels in a dose-dependent manner (50, 100 and 200 ng/anima...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(96)00709-1
更新日期:1996-12-12 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90067-8
更新日期:1989-07-18 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.09.047
更新日期:2008-12-03 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90695-m
更新日期:1991-11-05 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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更新日期:1986-04-29 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2011.08.048
更新日期:2011-11-16 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(83)90398-9
更新日期:1983-03-18 00:00:00
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journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
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更新日期:2001-06-08 00:00:00
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journal_title:European journal of pharmacology
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90214-q
更新日期:1990-08-21 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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更新日期:1993-11-09 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90088-3
更新日期:1985-07-31 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90100-5
更新日期:1982-07-16 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90127-3
更新日期:1982-02-05 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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更新日期:2020-12-15 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(84)90263-2
更新日期:1984-07-13 00:00:00
abstract::The role of flexibility of the alkyl side chain in the tetrahydrocannabinols to cannabinoid activity has been delineated in previous studies with side chain analogs of Delta(8)-tetrahydrocannabinol with double or triple bonds. This study investigated the site of antinociceptive action for these analogs through analysi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(00)00259-4
更新日期:2000-06-02 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
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更新日期:2013-12-05 00:00:00