INT1375
From wiki-pain
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Sentences Mentioned In
Key: | Protein | Mutation | Event | Anatomy | Negation | Speculation | Pain term | Disease term |
Dysregulation of ghrelin secretion and ghrelin resistance in the appetite control system occurred in aged mice and that rikkunshito ameliorated aging-anorexia via inhibition of PDE3. | |||||||||||||||
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In rat brain homogenate, these xanthines inhibit cyclic AMP phosphodiesterase. | |||||||||||||||
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In order to study the mode of action of flavoxate, the following activities were investigated: calcium blocking, inhibition of cyclic AMP phosphodiesterase (PDE), local anaesthetic activity, the effects on the synthesis and release of prostaglandins. | |||||||||||||||
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The antispasmodic activity of a drug can be correlated with inhibition of cyclic AMP phosphodiesterase, and since papaverine is a potent PDE inhibitor, we tested flavoxate for this activity. | |||||||||||||||
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Moreover, rikkunshito is also an enhancement of ghrelin receptor reactivity via PDE3 inhibition. | |||||||||||||||
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Dihydropyridine Ca-antagonists like nicardipine are also potent inhibitor of cyclic AMP phosphodiesterase. | |||||||||||||||
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Since IBMX mimicked the effect of nicardipine, the effect of a low dose of i.c.v. nicardipine in attenuating the hypotensive and bradycardic effects of i.c.v. clonidine may be mediated by inhibition of cyclic AMP phosphodiesterase in the central nervous system. | |||||||||||||||
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Nicardipine, in a dose of 0.3 microgram/kg/min for 60 min i.v., did not modulate the hypotensive and bradycardic effects of i.c.v. clonidine. 3-Isobutyl-l-methylxanthine (IBMX), a cyclic AMP phosphodiesterase inhibitor, in a dose of 3 micrograms/kg/min for 60 min i.c.v., also attenuated the hypotensive and bradycardic effects of i.c.v. clonidine. | |||||||||||||||
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Furthermore, PASMC receiving the combination of a PDE3 and a PDE4 inhibitor exhibited a significant additive or synergistic anti-mitogenic effect as compared to each PDE inhibitor used on its own. | |||||||||||||||
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NT-702 selectively inhibited PDE3 (IC(50)=0.179 and 0.260 nM for PDE3A and 3B) more potently than cilostazol (IC(50)=231 and 237 nM for PDE3A and 3B) among recombinant human PDE1 to PDE6. | |||||||||||||||
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Administered as an intracorporal injection, papaverine is a non-selective inhibitor of PDE3 and its isoforms (Carson 2007). | |||||||||||||||
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However, PDE4 inhibitors only weakly suppressed spontaneously generated tone, or contractions of isolated human airways smooth muscle in response to allergen, LTC4, and histamine, although this functional antagonism is significant when combined with a PDE3 inhibitor (Schmidt et al 2000). | |||||||||||||||
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Arteriopathy is a condition associated with arterial necrosis and has been observed in rats after treatment with large doses of many vasodilators including PDE3 and PDE4 inhibitors, adenosine agonists, endothelin receptor antagonists and potassium channel openers (Spina 2004). | |||||||||||||||
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Whilst macrophages do express PDE4 it appears that their function is poorly inhibited by PDE4 inhibitors, although the efficacy of these drugs is enhanced when used in combination with agents that raise intracellular levels of cyclic AMP (eg, prostaglandin E2) or if there is concurrent inhibition of PDE3 and PDE7 (Hatzelmann and Schudt 2001; Smith et al 2004). | |||||||||||||||
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General Comments
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