Disease relevance of epinine

• Arrhythmia scores were higher during ouabain than in control (p < 0.01) and in epinine treated hearts (p < 0.01); pretreatment with epinine did not modify arrhythmia score during ouabain administration [1].
• Epinine is a cardiovascular agent used in congestive heart failure because of its dopaminergic and adrenoreceptor agonist properties [2].
• The high level of epinine in one patient was associated with severe hypertension and tachycardia [3].
• As the kinetics of ibopamine's active moiety, free epinine, were not apparently altered by chronic renal failure, adjustment of its dosage should not be necessary in renal diseases [4].

Psychiatry related information on epinine

• Ergometrine, epinine, (+/-)-2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronapthalene hydrobromide (ADTN), 1,2,3,4-tetrahydro-6,7,-dihydroxyisoquinoline hydrochloride (THIQ), muscimol and glycine elicited locomotor activity when injected into the substantia nigra pars reticulata bilaterally [5].

High impact information on epinine

• Contrary to previous reports, 5-methyltetrahydrofolic acid does not mediate the methylation of dopamine to epinine [6].
• The effects of DA, and the DA receptor agonists epinine and apomorphine were determined [7].
• The DA agonists relaxed the smooth muscle strips in the following order of potency: DA greater than epinine greater than apomorphine [7].
• Dopamine and epinine caused a dose-related fall in basal LES muscle tension and in amplitude of EB muscle "off" responses [8].
• Epinine induced a reduction of left ventricular end diastolic pressure (p < 0.01) and a rise in left ventricular developed pressure (p < 0.01) but both effects decreased progressively with aging [1].

Chemical compound and disease context of epinine

• Dopamine has been widely utilized in the treatment of acute congestive heart failure, ibopamine, the diisobutyrate ester of N-methyldopamine (epinine), is a novel inotropic agent that, unlike-dopamine, is orally active [9].

Biological context of epinine

• From dose-response curves it was demonstrated that epinine produced an increase in amplitude and duration of the plateau, and in duration of the action potential [10].
• The cyclic voltammometric behavior of epinephrine, norepinephrine, dopamine, epinine, alpha-methyldopamine, beta-methyldopamine, beta-methylepinine, and beta-methoxyepinine has been examined in order to evaluate substituent effects on cyclization rates of the electrochemically generated quinones [11].
• 3. Epinine increased aortic blood flow (AoBF, 24 +/- 6%), which was due to an increase in heart rate (HR) for doses less than 10 micrograms kg-1 min-1 [12].
• Comparison of the alpha adrenoceptor activity of dopamine, ibopamine and epinine in the pulmonary circulation of the dog [13].
• The addition of (R)-sulpiride, a DA antagonist, abolished DA and epinine-induced vasodilation in the mesenteric and renal vascular beds [14].

Anatomical context of epinine

• The permeabilities of epinine and the diester prodrugs through endothelial cell monolayers grown on porous supports were related to their lipophilicity and molecular weight [15].
• Cardiac inotropic as well as coronary and pulmonary artery actions of epinine in human isolated tissues [16].
• On the other hand, apomorphine and epinine were less potent while dopamine was more potent in the medial basal hypothalamus [17].
• Only in nonfailing myocardium, epinine increased force of contraction as effectively as Ca++ [16].
• In human coronary artery rings and pulmonary artery rings epinine alone as well as epinine in the presence of propranolol initiated a concentration-dependent increase in tension development in precontracted (prostaglandin F2 alpha, 0.3 mumol/l) as well as in non-precontracted rings [16].

Associations of epinine with other chemical compounds

• The positive inotropic effect of epinine was mediated only by myocardial beta-adrenoceptor stimulation; over the whole range of concentrations, the inotropic action of epinine was not influenced by phentolamine (3.10(-6) mol . litre-1), but was inhibited by propranolol (3.10(-8) mol . litre-1) [10].
• Effect of ibopamine and the active metabolite epinine on the catecholamine content of rat hypothalamus and brainstem in vitro [18].
• Epinine concentration-dependently relaxed isolated precontracted (PGF2 alpha) human renal artery rings (P < 0.05) in the presence of phentolamine, as effectively (epinine -30 +/- 4 mN, dopamine -31 +/- 5 mN) and with the same potency as dopamine (epinine EC50 0.7 mumol/l (0.4-1.2 mumol/l), dopamine 0.5 mumol/l (0.2-1.7 mumol/l) [19].
• Epinine was extracted from human plasma and urine via an alumina adsorption procedure; this procedure was also used to estimate epinine conjugates after prior enzymatic hydrolysis [2].
• Domperidone did not affect dopamine- and epinine-evoked blood pressure- and heart rate-changes, but antagonized their prolactin-effects (at least at the lower doses) [20].

Gene context of epinine

• The results of this study show that epinine is a substrate for both forms of MAO in rat liver, although the contribution of MAO A to the deamination of this secondary amine appears to be slightly more important than that of MAO B [21].
• Epinine exerted higher affinity at beta-2 compared to beta-1 adrenoceptors in radioligand binding experiments ([125I]iodocyanopinodolol) [16].
• 1. The effects of epinine or dopamine (both 1-10 micrograms kg-1 min-1) on systemic haemodynamics and plasma concentrations of catecholamines and prolactin were studied in conscious pigs before and after combined non-selective alpha- and beta-adrenoceptor blockade [12].
• Lack of epinine formation in adrenal medulla and brain of rats during cold exposure and inhibition of dopamine beta-hydroxylase [22].
• Kinetic study of the transient phase of a chemical reaction system coupled to an enzymatically catalyzed step. Application to the oxidation of epinine by tyrosinase [23].

Analytical, diagnostic and therapeutic context of epinine

• Sodium was measured by ion specific electrode and dopamine by HPLC with electrochemical detection (using epinine as an internal standard) [24].
• These methods were used to study the pharmacokinetics and metabolic fate of epinine after oral administration of ibopamine to healthy volunteers [2].
• Quantitative analytical methods, using high-performance liquid chromatography coupled with electrochemical detection, were developed for the determination of epinine and its known metabolites in biological media [2].
• The effect of the timing of a standard meal relative to a single oral dose of 200 mg ibopamine, on the appearance of its pharmacologically active metabolite, epinine, in plasma was investigated in a randomised crossover study in 12 healthy volunteers [25].
• Endogenous synthesis of N-methylnorsalsolinol in rat brain during in vivo microdialysis with epinine [26].

References