Abstract：
:Mastoparan activated membrane-bound guanylate cyclase and potentiated the effect of atrial natriuretic factor (ANF) and ATP on guanylate cyclase activity in rat lung membranes. Mastoparan is a cationic, amphiphilic tetradecapeptide with an amidated carboxyl terminus. It takes the alpha-helical conformation upon interacting with the membrane. Several analogs were synthesized to study the role of the positive charges, the carboxyl amino group and the alpha-helical conformation of mastoparan in the activation of guanylate cyclase. The results showed that substitution of the C-terminal amide group of mastoparan with a carboxyl group significantly reduced its potency on the activation of guanylate cyclase. Replacement of three lysine residues of mastoparan with aspartic acid or serine residues completely abolished the stimulatory effect of mastoparan. When the alanine at position 10 of mastoparan was substituted by a proline, the resulting analog had no effect on guanylate cyclase activity. These results demonstrate that the positive charges and the helical structure of mastoparan are critical determinants for the activation of guanylate cyclase.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Song DL,Chang GD,Ho CL,Chang CHdoi
10.1016/0922-4106(93)90196-gsubject
Has Abstractpub_date
1993-11-15 00:00:00pages
283-8issue
3eissn
0014-2999issn
1879-0712journal_volume
247pub_type
杂志文章abstract：:Recombinant vaccinia viruses harboring the human dopamine D4 receptor cDNA containing two 48 base pair-repeats (D4.2) or the rat dopamine D2 short (D2s) receptor cDNA were used to infect rat-1 fibroblasts. Heterologous expression of both dopamine receptors was demonstrated in binding assays. The affinity constants of ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(95)90011-x
更新日期：1995-06-23 00:00:00
abstract：:27-O-Caffeoyl myricerone (50-235) is a nonpeptide endothelin receptor antagonist which is highly selective for the endothelin ETA receptor subtype. In order to determine which functional groups in 50-235 are essential for its activity, we examined the potencies of 50-235 and its derivatives to inhibit [125I]endothelin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(93)90081-j
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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(87)90186-5
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abstract：:The potential of resiniferatoxin and capsaicin to modulate emesis and genital grooming was investigated in Suncus murinus. Resinifertoxin (3-30 nmol, i.c.v.), E-capsaicin (10-100 nmol, i.c.v.) and Z-capsaicin (100 nmol, i.c.v.) induced emesis (P<0.05) and subsequently antagonised the emetic response induced by intraga...
journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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doi：10.1016/0014-2999(88)90486-4
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)00657-s
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abstract：:The present paper describes a theoretical study on the mechanism underlying the reaction of cellular glutathione (GSH) with polyunsaturated fatty acid ozonides. The reaction can be catalyzed by glutathione S-transferases and leads to detoxication of the ozonides. Semi-empirical molecular orbital computer calculations ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0926-6917(92)90031-7
更新日期：1992-12-01 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90429-8
更新日期：1987-06-19 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：2006-10-24 00:00:00
abstract：:We recently observed that the 5-hydroxytryptamine (5-HT)(1A) receptor antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)-cycloh exanecarboxamide (WAY 100635) enhanced antipsychotic-induced catalepsy, which we hypothesized to be due to a blockade of tonic 5-HT(1A) receptor activation. Here, we ex...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00178-3
更新日期：2000-04-28 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.12.003
更新日期：2013-01-30 00:00:00
abstract：:Selective serotonin reuptake inhibitors (SSRIs) are widely used as a first-line therapy in postpartum depression. The objective of this study was to determine the mechanism underlying the inhibitory effects of the SSRI, fluvoxamine, on β-casein expression, an indicator of lactation, in MCF-12A human mammary epithelial...
journal_title：European journal of pharmacology
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doi：10.1016/j.ejphar.2015.09.038
更新日期：2015-11-05 00:00:00
abstract：:The pharmacological profile of a novel and newly discovered non-steroidal anti-inflammatory and analgesic compound, 3-(difluoromethyl)-1-(4-methoxyphenyl)-5-[4-(methylsulfinyl)phenyl]pyraz ole (FR140423), was investigated. In recombinant human cyclooxygenase enzyme assays, the inhibition of prostaglandin E2 formation ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00868-1
更新日期：1999-01-22 00:00:00
abstract：:Endogenous cannabinoid ligands and cannabinoid CB(1) receptor agonists have been shown to exert potent anticonvulsant effects in various experimental models of epilepsy. The purpose of this study was to determine the effects of arachidonyl-2'-chloroethylamide (ACEA; N-(2-chloroethyl)-5Z,8Z,11Z,14Z-eicosatetraenamide, ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.07.037
更新日期：2006-10-10 00:00:00
abstract：:Natural purines like ATP, ADP and adenosine have crucial roles in platelet physiology. This knowledge has been significant in drug development and today ADP receptor antagonists are widely used for prevention of thrombotic events following myocardial infarction and ischaemic stroke. Recent studies have shown that a pu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172428
更新日期：2019-08-15 00:00:00
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journal_title：European journal of pharmacology
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更新日期：2000-08-18 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
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更新日期：1995-06-06 00:00:00
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journal_title：European journal of pharmacology
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doi：10.1016/0014-2999(89)90257-4
更新日期：1989-05-30 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90701-3
更新日期：1994-05-12 00:00:00
abstract：:The characteristics of beta-adrenoceptors on frog and chick erythrocytes have been compared to those present on rat erythrocyte, lung and cerebral cortical membranes. The receptors have been examined using the specific ligand [3H]dihydroalprenolol ([3H]DHA) with conventional filtration techniques. The equilibrium diss...
journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1981-08-27 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.07.042
更新日期：2016-10-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)94796-z
更新日期：1990-03-13 00:00:00
abstract：:The LTD4 antagonist, Wy-48,252 (1,1,1-trifluoro-N-[3-(2-quinolinylmethoxy)phenyl]methanesulfonamide), was assessed for its ability to modulate arachidonic acid metabolism in several inflammatory cells. In A23187-stimulated rat neutrophils, Wy-48,252 effectively inhibited the conversion of exogenous [14C]arachidonic ac...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90462-1
更新日期：1988-03-22 00:00:00
abstract：:Coronary artery disease (CAD) is the most common cause of sudden death, and death of people over 20 years of age. Because ozone therapy can activate the antioxidant system and improve blood circulation and oxygen delivery to tissue, the aim of this study was to investigate the therapeutic efficacy of ozone in patients...
journal_title：European journal of pharmacology
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.ejphar.2012.07.010
更新日期：2012-09-15 00:00:00
abstract：:Purinergic P2Y-receptor agonists amplify glucose-induced insulin secretion from pancreatic beta-cells, thus offering new opportunities for the treatment of type 2 diabetes. However, little is known about which subtypes of purinergic P2Y receptors are expressed in these cells. The INS-1 beta-cell line is used as a mode...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.04.012
更新日期：2007-07-30 00:00:00
abstract：:Due to the limited results achieved in the clinical treatment of heart failure, a new inotropic strategy of myosin motor activation has been developed. The lead molecule of myosin activator agents is omecamtiv mecarbil, which binds directly to the heavy chain of the cardiac β-myosin and enhances cardiac contractility ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.05.027
更新日期：2017-08-15 00:00:00
abstract：:The ability of isoproterenol to relax guinea-pig trachea was examined in tissues precontracted with three concentrations of methacholine or three corresponding equieffective concentrations of leukotriene D4. Although increasing the concentration of either contractile agent progressively shifted isoproterenol concentra...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90580-6
更新日期：1984-07-20 00:00:00
abstract：:This study investigates the effect and the underlying mechanism of 2',3-dihydroxy-5-methoxybiphenyl (RIR-2), a lignan extracted from the roots of Rhaphiolepis indica (L.) Lindl. ex Ker var. tashiroi Hayata ex Matsum. & Hayata (Rosaceae), on N-formyl-L-methionyl-L-leucyl-L-phenylalanine (fMLP)-induced respiratory burst...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.03.037
更新日期：2018-06-15 00:00:00
