methyldopamine การใช้

• However, the story complicates as alpha-methyldopamine readily oxidizes to the o-quinone and reacts with endogenous antioxidants in the body, such as glutathione ( GSH ).
• Bioassay-guided fractionation of the methanolic extract of " M . jalapa " also led to the isolation of an active polyphenolic amide : N-trans-feruloyl 42-O-methyldopamine.
• When dopamine or " N "-methyldopamine were injected directly into the nucleus accumbens of mice, however, doses of 12.5-50 ?g produced marked hyperactivity, with the latter being somewhat more potent.
• It is also now generally accepted that MDMA neurotoxicity results from a variety of different causes and is not solely due to accumulation of alpha-methyldopamine, making it unclear how much less neurotoxic DFMDA and related drugs would be in practice.
• Small amounts of metabolites ( alpha-methyldopa and alpha-methyldopamine ) were found after the administration of both single-doses and maintenance-doses of AMPT . Small amounts of methyltyramine and alpha-methylnoradrenaline were found in patients undergoing AMPT therapy.
• "' Deoxyepinephrine "', also known by the common names "'N-methyldopamine "'and "'epinine "', is an organic compound and natural product that is structurally related to the important neurotransmitters dopamine and epinephrine.
• It was demonstrated by Miller, et al . ( 1997 ), that 5-( glutathion-S-yl )-alpha-methyldopamine and 5-( N-acetylcystein-S-yl )-alpha-methyldopamine produced similar effects to the parent compound, but did not induce neurotoxicity.
• It was demonstrated by Miller, et al . ( 1997 ), that 5-( glutathion-S-yl )-alpha-methyldopamine and 5-( N-acetylcystein-S-yl )-alpha-methyldopamine produced similar effects to the parent compound, but did not induce neurotoxicity.
• Another related compound however, 2, 5-bis-( glutathion-S-yl )-alpha-methyldopamine, did in fact induce neurotoxicity, providing initial evidence that this metabolite may be the source of neuronal toxicity following the administration of MDA and MDMA, and the subsequent reduction in 5-HT ( Serotonin ) axons.
• It was first demonstrated, in 1978, by Conway, " et al . " and possibly others that, while alpha-methyldopamine caused acute decreases in the levels of neuronal dopamine, in some areas of the brain in excess of 75 %, levels returned to baseline within 12 hours, indicating that alpha-methyldopamine would not be responsible for the toxic effects observed.
• It was first demonstrated, in 1978, by Conway, " et al . " and possibly others that, while alpha-methyldopamine caused acute decreases in the levels of neuronal dopamine, in some areas of the brain in excess of 75 %, levels returned to baseline within 12 hours, indicating that alpha-methyldopamine would not be responsible for the toxic effects observed.
• Receptor binding studies, in competition with [ 3 H ]-spiperone, using receptors from pig anterior pituitary, have revealed the following affinities for D 2 receptors exhibited by DMDA : K a high = 20 nM; K a low = 10200 nM . In comparison, the corresponding affinities for " N "-methyldopamine are : 10.4 nM ( high ) and 3430 nM ( low ), while for dopamine they are 7.5 nM ( high ) and 4300 nM ( low affinity state ).
• "' Difluoromethylenedioxyamphetamine "'( "'DiFMDA "') is a substituted derivative of 3, 4-methylenedioxyamphetamine ( MDA ), which was developed by Daniel Trachsel and coworkers, along with the corresponding fluorinated derivatives of MDMA, MDEA, BDB and MBDB, with the aim of finding a non-neurotoxic drug able to be used as a less harmful substitute for entactogenic drugs such as MDMA . Since a major route of the normal metabolism of these compounds is scission of the methylenedioxy ring, producing neurotoxic metabolites such as alpha-methyldopamine, it was hoped that the difluoromethylenedioxy bioisostere would show increased metabolic stability and less toxicity.