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《Journal of receptor and signal transduction research》2013,33(5):381-386
The present study was undertaken to ascertain whether the casein derived bitter tastant Cyclo (Leu-Trp) [CLT] has an affinity or not for the particular receptors of the pineal hormone, melatonin, on the melanophores of a major carp Labeo rohita (Ham.). The bitter tastant CLT, in the dose range of 3.34?×?10?16 M to 3.34?×?10?4 M, has induced an aggregatory effect but not in a dose dependent manner. Binding of CLT with the receptors may vary at different concentrations. Denervation of the melanophores has shown a complete inhibition of the CLT mediated aggregation. Prazosin has partially inhibited the aggregatory effect of CLT. Moreover, the bitter tastant’s response is mediated through the α2 adrenoceptors only at particular dose ranges. The MT1 and MT2 melatonin receptor antagonist luzindole and the MT2 specific antagonist K185 have perfectly blocked the aggregatory effects of CLT. We have found that the CLT mediated aggregatory effect is dependent upon the release of neurotransmitters and the two subtypes of melatonin (MT) receptors (MT1 and MT2) possess a perfect affinity towards the bitter tastant CLT. Our study demands a need to further make a clinical research on the effects of bitter tastants on the physiology of the biological rhythm maintaining hormone melatonin. 相似文献
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Nineteen indole alkaloids were isolated from Ghanaian Rauwolfia vomitoria leaves. The alkaloids comprised E-seco indole, sarpagan, picrinine, akuammiline, heteroyohimbine, oxindole, yohimbine and indolenine types. The biosynthetic relationship of the alkaloids is discussed. 相似文献
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22 indole alkaloids were isolated from the stem bark of Nigerian Rauwolfia vomitoria and 20 characterized. The alkaloids comprised E-seco heteroyohimbine, sarpagan, dihydroindole, yohimbine and heteroyohimbine types. The biosynthetic relationship of the alkaloids is discussed. 相似文献
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24 indole alkaloids were isolated from the stem bark of Rauwolfia cumminsii and 21 identified. The alkaloids comprised E-seco, sarpagan, dihydroindole, yohimbine, heteroyohimbine, 18-hydroxyyohimbine ester and anhydronium types together with peraksine and deacetylpicraline. The probable biosynthesis of the alkaloids is discussed. 相似文献
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James P. Kutney Lewis S.L. Choi Pawel Kolodziejczyk Stephen K. Sleigh Kenneth L. Stuart Brian R. Worth W.G.W. Kurz K.B. Chatson F. Constabel 《Phytochemistry》1980,19(12):2589-2595
A detailed study of one cell line (coded as 943) of Catharanthus roseus cell cultures has revealed the presence of the following alkaloids: ajmalicine, vallesiachotamine, hörhammerinine, hörhammericine, vindolinine, 19-epi- vindolinine, 19-acetoxy-11-methoxytabersonine, 19-acetoxy-11 -hydroxytabersonine, 19-hydroxy- 11-methoxytabersonine, yohimbine and isositsirikine, together with dimethyltryptamine and a new strychnos-type alkaloid. 相似文献
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Mauricio Ibacache Gina Sanchez Zully PedrozoFelipe Galvez Claudio Humeres Ghislaine EchevarriaJuan Duaso Mario Hassi Lorena GarciaGuillermo Díaz-Araya Sergio Lavandero 《生物化学与生物物理学报:疾病的分子基础》2012,1822(4):537-545
Pharmacological preconditioning limits myocardial infarct size after ischemia/reperfusion. Dexmedetomidine is an α2-adrenergic receptor agonist used in anesthesia that may have cardioprotective properties against ischemia/reperfusion injury. We investigate whether dexmedetomidine administration activates cardiac survival kinases and induces cardioprotection against regional ischemia/reperfusion injury. In in vivo and ex vivo models, rat hearts were subjected to 30 min of regional ischemia followed by 120 min of reperfusion with dexmedetomidine before ischemia. The α2-adrenergic receptor antagonist yohimbine was also given before ischemia, alone or with dexmedetomidine. Erk1/2, Akt and eNOS phosphorylations were determined before ischemia/reperfusion. Cardioprotection after regional ischemia/reperfusion was assessed from infarct size measurement and ventricular function recovery. Localization of α2-adrenergic receptors in cardiac tissue was also assessed. Dexmedetomidine preconditioning increased levels of phosphorylated Erk1/2, Akt and eNOS forms before ischemia/reperfusion; being significantly reversed by yohimbine in both models. Dexmedetomidine preconditioning (in vivo model) and peri-insult protection (ex vivo model) significantly reduced myocardial infarction size, improved functional recovery and yohimbine abolished dexmedetomidine-induced cardioprotection in both models. The phosphatidylinositol 3-kinase inhibitor LY-294002 reversed myocardial infarction size reduction induced by dexmedetomidine preconditioning. The three isotypes of α2-adrenergic receptors were detected in the whole cardiac tissue whereas only the subtypes 2A and 2C were observed in isolated rat adult cardiomyocytes. These results show that dexmedetomidine preconditioning and dexmedetomidine peri-insult administration produce cardioprotection against regional ischemia/reperfusion injury, which is mediated by the activation of pro-survival kinases after cardiac α2-adrenergic receptor stimulation. 相似文献
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Serotonin (5-hydroxytryptamine, 5-HT) plays a key role in modulating diverse physiological processes and behaviors in both protostomes and deuterostomes. These functions are mediated through the binding of serotonin to its receptors, which are recognized as potential insecticide targets. We investigated the sequence, pharmacology and tissue distribution of three 5-HT receptors (Piera5-HT1A, Piera5-HT1B, Piera5-HT7) from the small white butterfly Pieris rapae, an important pest of cultivated cabbages and other mustard family crops. Activation of Piera5-HT1A or Piera5-HT1B by 5-HT inhibited the production of cAMP in a dose-dependent manner. Stimulation of Piera5-HT7 with 5-HT increased cAMP level significantly. Surprisingly, with the exception of 5-methoxytryptamine, agonists including α-methylserotonin, 8-Hydroxy-DPAT and 5-carboxamidotryptamine activated these receptors poorly. The results are consistent with previous findings in Manduca sexta. All three receptors were blocked by methiothepin, but ketanserin and yohimbine were not effective. The selective mammalian 5-HT receptor antagonists SB 216641 and SB 269970 displayed potent inhibition effects on Piera5-HT1B and Piera5-HT7 respectively. The results we achieved here indicate that the pharmacological properties of Lepidoptera 5-HT receptors are quite different from those in other insects and vertebrates and may contribute to development of new selective pesticides. This study offers important information on three 5-HT receptors from P. rapae that will facilitate further analysis of the functions of 5-HT receptors in insects. 相似文献