Effect of Docarpamine, a Novel Orally Active Dopamine Prodrug, on the Formation of Free and Sulfoconjugated Dopamine in Patients Who Underwent Cardiac Surgery

Tano, Kazutoshi; Yoshizumi, Masanori; Kitagawa, Tetsuya; Hori, Takaki; Kitaichi, Takashi; Itoh, Kotaro; Katoh, Itsuo

doi:10.1016/s0024-3205(97)00706-6

Cited by 2 publications

(1 citation statement)

References 26 publications

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“…Docarpamine, [ N -( N -acetyl-L-methionyl)- O , O - bis (ethoxycarbonyl)dopamine), 2 ], a pseudopeptide prodrug of dopamine, is administered orally in the treatment of renal and cardiovascular pathologies [ 15 , 16 ].…”

Section: Prodrugs That Rely (Mostly) On Enzymatic Activationmentioning

confidence: 99%

Prodrugs for Amines

2008

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The purpose of this work is to review the published strategies for the production of prodrugs of amines. The review is divided in two main groups of approaches: those that rely on enzymatic activation and those that take advantage of physiological chemical conditions for release of the drugs. A compilation of the most important approaches is presented in the form of a table, where the main advantages and disadvantages of each strategy are also referred.

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Section: Prodrugs That Rely (Mostly) On Enzymatic Activationmentioning

confidence: 99%

Prodrugs for Amines

2008

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Effect of Sarpogrelate Hydrochloride, A 5-HT2 Blocker, on Insulin Resistance in Otsuka Long-Evans Tokushima Fatty Rats (OLETF rats), A Type 2 Diabetic Rat Model

Takishita

Takahashi²,

Harada³

et al. 2004

Journal of Cardiovascular Pharmacology

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5-hydroxytryptamine (5-HT) is closely related to pathogenesis of angiopathy in type 2 diabetes. Acute and chronic effects of sarpogrelate hydrochloride (sarpogrelate), a 5-HT2 blocker, on glucose tolerance and insulin resistance were examined. Otsuka Long-Evans Tokushima Fatty (OLETF) rats, a model of type 2 diabetes, were randomly assigned to 2 groups; those with 30 mg/kg BW/d sarpogrelate treatment of 4 weeks (HTB group) and without (control group). The glucose infusion rate was significantly increased in the HTB group compared with the control group. The blood glucose levels after oral glucose tolerance test and levels of plasma insulin and lipids were significantly lower in the HTB group than in the control group. To investigate mechanism of the improvement by sarpogrelate, acute effect of 5-HT and its blocking effect by sarpogrelate on blood levels of glucose were examined in 25-week-old Sprague-Dawley rats. Blood glucose levels were significantly increased by administration of 5-HT. This increase was reversed by pretreatment of sarpogrelate. A plasma adrenaline level also rose significantly by injection of the 5-HT and was prevented by pretreatment of sarpogrelate. These results indicate that sarpogrelate improves insulin resistance in type 2 diabetic rats.

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Effect of Docarpamine, a Novel Orally Active Dopamine Prodrug, on the Formation of Free and Sulfoconjugated Dopamine in Patients Who Underwent Cardiac Surgery

Cited by 2 publications

References 26 publications

Prodrugs for Amines

Prodrugs for Amines

Effect of Sarpogrelate Hydrochloride, A 5-HT2 Blocker, on Insulin Resistance in Otsuka Long-Evans Tokushima Fatty Rats (OLETF rats), A Type 2 Diabetic Rat Model

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