Abstract：
:The action of a novel 5-HT3 receptor antagonist, AS-5370, has been studied on two electrophysiological models for 5-HT3 receptors: whole-cell patch-clamp recordings from mouse neuroblastoma-rat glioma (NG108-15) cells and grease-gap recordings from rat isolated vagus nerve. The 5-hydroxytryptamine (5-HT)-induced fast inward current of voltage-clamped NG108-15 cells was antagonized by 1 nM AS-5370 in an insurmountable manner. On the rat vagus, AS-5370 reduced the maximum depolarizing response to 5-HT in a concentration-dependent manner. The IC50 for AS-5370 on the rat vagus was 0.3-1.0 nM. The EC50 for 5-HT on the rat vagus was not appreciably affected by AS-5370. On the rat vagus, the (R) enantiomer of AS-5370 was about 30 times more potent than the (S) enantiomer. The antagonist action of AS-5370 on these two cell types was compared with that of (+)-tubocurarine. Unlike tubocurarine, the effect of AS-5370 on NG108-15 cells was not readily reversed during wash. On the rat vagus, tubocurarine antagonized in a competitive manner with an IC50 of 0.3-1.0 microM (pKb = 7.2). It is concluded that AS-5370 is a potent 5-HT3 receptor antagonist on both NG108-15 cells and the rat vagus, but it does not act in a competitive manner.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Newberry NR,Sprosen TS,Watkins CJ,Leslie RA,Grahame-Smith DGdoi
10.1016/0014-2999(92)90591-qkeywords:
subject
Has Abstractpub_date
1992-08-14 00:00:00pages
135-40issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(92)90591-Qjournal_volume
219pub_type
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journal_title：European journal of pharmacology
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更新日期：1992-01-14 00:00:00
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journal_title：European journal of pharmacology
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doi：10.1016/0922-4106(91)90037-i
更新日期：1991-07-12 00:00:00
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journal_title：European journal of pharmacology
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pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.07.018
更新日期：2005-10-03 00:00:00
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journal_title：European journal of pharmacology
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更新日期：2004-03-08 00:00:00
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更新日期：2012-06-05 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
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pub_type： 杂志文章,评审
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更新日期：2014-10-15 00:00:00
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journal_title：European journal of pharmacology
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更新日期：2009-08-15 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：2006-07-01 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：1997-03-19 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)94111-a
更新日期：1990-11-06 00:00:00
abstract：:Rat anococcygeus muscles were isolated 4 h after treatment with either E. coli endotoxin (20 mg kg-1 i.p.) or saline. The contractile responses of the muscle to electrical field stimulation, and to the alpha 1-adrenoceptor agonist cirazoline were impaired by endotoxin treatment. Inhibition of the L-arginine pathway wi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90285-x
更新日期：1991-09-24 00:00:00
