The causal role of PAF and leukotrienes in acute cardiac allograft rejection in rats

Foegh, Marie L.; Khirabadi, Bijan S.; Rowles, John R.; Braquet, P.; Ramwell, Peter W.

doi:10.1016/0031-6989(86)90045-7

Cited by 9 publications

(4 citation statements)

References 15 publications

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“…Another presumed beneficial effect of BN 52021 in cardiac diseases is the prevention of delayed hypersensitivity reactions occurring in cardiac transplantation. The treatment of rat cardiac allograft recipients with BN 52021, in combination either with azatioprine or cyclosporine A, significantly delays graft rejection (33,34). Moreover, in combination with other PAF receptor antagonists, BN 52021 improves allograft survival to the same extent as prednisolone (50).…”

Section: In Vitro Biochemical and Functional Studiesmentioning

confidence: 99%

Cardiovascular Properties of Yangambin, a Lignan Isolated from Brazilian Plants

Tibiriçá

2001

Cardiovascular Drug Reviews

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Yangambin was initially selected from a number of lignans isolated from Brazilian plants for its ability to antagonize Platelet-Activating Factor (PAF, 1-O-hexadecyl-2-acetyl-sn-glyceryl-3-phosphorylcholine)-induced biological effects. Subsequently it was shown that, besides its antagonistic properties at PAF receptors, yangambin also prevents the cardiovascular collapse observed during anaphylactic and endotoxic /septic shocks, as well as the vascular and cardiac hyporesponsiveness to catecholamines in endotoxic shock. It is suggested that this naturally occurring compound could be of potential interest in the adjunctive management of the above mentioned pathologies. In the present article, we review the main studies investigating the pharmacological properties of yangambin related to the cardiovascular function.

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Section: In Vitro Biochemical and Functional Studiesmentioning

confidence: 99%

Cardiovascular Properties of Yangambin, a Lignan Isolated from Brazilian Plants

Tibiriçá

2001

Cardiovascular Drug Reviews

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“…6-Bromohexanoate (7). 3-Hydroxy-2-methylenepropyl Noctadecylcarbamate (6) (1.62 g, 4.2 mmol), N,N'dicy clohexylcarbodiimide (1.08 g, 5.2 mmol), 4-(dimethylamino)pyridine (52 mg, 0.43 mmol), and 6-bromohexanoic acid (0.91 g, 4.7 mmol) were stirred in CH2C12 (50 mL) at 22 °C for 20 h. Ether (50 mL) was added, and the mixture was filtered.…”

Section: -Methylene-3-[[(octadecylamino)carbonyl]oxy]propylmentioning

confidence: 99%

Derivatives of 2-methylenepropane-1,3-diol as new antagonists of platelet activating factor

Grue-Sørensen¹,

Im²,

Ck³

1988

J. Med. Chem.

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Two new achiral platelet activating factor (PAF) antagonists, N-[5-[[2-methylene-3- [[(octadecylamino)carbonyl]oxy]propoxy]carbonyl]pentyl]pyridinium bromide and 3-[6-[[2-methylene-3- [[(octadecylamino)carbonyl]oxy]propoxy]carbonyl]hexyl]thiazolium bromide were synthesized from 2-methylenepropane-1,3-diol. Platelet aggregation in platelet-rich plasma from rabbits, induced by racemic C16-PAF, was competitively antagonized by 9 or 10. At concentrations less than or equal to 10(-4) M, neither compound 9 nor compound 10 caused platelet aggregation, nor did they inhibit platelet aggregation induced by collagen or adenosine diphosphate. Bronchoconstriction in the guinea pig and hypotension in the rat, induced by racemic C16-PAF, were also effectively antagonized by 9 and 10. Both appear to be more potent as PAF antagonists than Takeda's CV-3988.

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“…U s a g e b y a n y i n d i v i d u a l n o t d i r e c t l y a s s o c i a t e d w i t h s c i t e i s p r o h i b i t e d .TableII. Partition Coefficients compd log Papp°a t pH7Partition coefficient log Papp was determined between 1-octanol and an aqueous buffer solution at pH 7.4 (25 °C).…”

mentioning

confidence: 99%

Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine

Eberlein¹,

Engel²,

Trummlitz³

et al. 1988

J. Med. Chem.

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In order to gain some insight into those structural features that control M1 selectivity, a selected set of pirenzepine analogues has been studied in which both the tricyclic ring system and the basic side chain have been varied. Binding studies were conducted in rat tissue homogenates from cerebral cortex (M1) and gastric fundus (M2). The ratio of IC50 values of the test compounds in the two different tissues was taken as a measure of M1 receptor selectivity. Several derivatives, especially those with flexible side chains, i.e. high degree of freedom of rotation around single bonds, proved to be nonselective. Among semirigid compounds only those containing 6-membered ring systems (11, 13, 14, and 15) showed significant M1 selectivity. Principles of structure-activity and structure-selectivity are discussed.

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The causal role of PAF and leukotrienes in acute cardiac allograft rejection in rats

Cited by 9 publications

References 15 publications

Cardiovascular Properties of Yangambin, a Lignan Isolated from Brazilian Plants

Cardiovascular Properties of Yangambin, a Lignan Isolated from Brazilian Plants

Derivatives of 2-methylenepropane-1,3-diol as new antagonists of platelet activating factor

Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine

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