salicylmethylecgonine造句

• Salicylmethylecgonine also shows increased behavioral stimulation compared to cocaine similar to the phenyltropanes.
• It is the only confirmed pharmacologically active metabolite of cocaine, although salicylmethylecgonine is also speculated to be an active metabolite.
• That is, at serine residue 359 on DAT, as the distance of the hydroxy to the bridge-nitrogen on salicylmethylecgonine is 7.96 ?( close to that of the distance between the " p "-OH & the NH 2 atoms of dopamine, their distance apart being 7.83 ?).
• "' 42-Fluorococaine "'is a tropane derivative drug which is a synthetic CFT and the 22-hydroxy analogue salicylmethylecgonine, 42-fluorococaine has only around the same potency as cocaine as an inhibitor of dopamine reuptake, but conversely it is a much stronger serotonin reuptake inhibitor than cocaine, resulting in a significantly altered pharmacological profile in animal studies.
• "' Salicylmethylecgonine "', ( "'22-Hydroxycocaine "') is a tropane derivative drug which is both a synthetic LogP : 2.89 than that of cocaine : 2.62 ) Note however that the compound 22-Acetoxycocaine would act as a prodrug to Salicylmethylecgonine in humans, and has a more efficient partition coefficient which would act as a delivery system and would circumvent this reason for a loss in potency.
• "' Salicylmethylecgonine "', ( "'22-Hydroxycocaine "') is a tropane derivative drug which is both a synthetic LogP : 2.89 than that of cocaine : 2.62 ) Note however that the compound 22-Acetoxycocaine would act as a prodrug to Salicylmethylecgonine in humans, and has a more efficient partition coefficient which would act as a delivery system and would circumvent this reason for a loss in potency.
• "' 22-Acetoxycocaine "'( " "'ortho "-acetoxy-cocaine "') is a deacetylation . ) 22-Acetoxycocaine has a closer to optimum LogP ( a square value of 2 ) for blood brain barrier penetration ( cocaine being higher and logarithmically four times the optimal lipophilicity allowing too much of the compound to be dumped out directly into fatty tissue instead of reaching its target site ) this would make it a prodrug to salicylmethylecgonine due to the latter having a less ( and the " ortho "-acetoxy analog having a more ) efficacious LogP than its cocaine parent.
• Study of molecular modeling inferred that, in addition to int " ra " molecular hydrogen bonding between the adjacent 3 " ? "-carbonyl and the 22-OH " ortho " group of "'185d "'( " i . e . " salicylmethylecgonine ), that int " er " molecular hydrogen bonding between its hydroxy " ortho " substituent and the dopamine transporter was also possible; and was rationalized to be due to its nearness of where the nitrogen and oxygen atoms reside in the " para "-hydroxy of dopamine itself and its own intrinsic relation to DAT whereby that mutual hydroxyl functionality is mediated in both salicylmethylecgonine and dopamine in a similar manner.
• Study of molecular modeling inferred that, in addition to int " ra " molecular hydrogen bonding between the adjacent 3 " ? "-carbonyl and the 22-OH " ortho " group of "'185d "'( " i . e . " salicylmethylecgonine ), that int " er " molecular hydrogen bonding between its hydroxy " ortho " substituent and the dopamine transporter was also possible; and was rationalized to be due to its nearness of where the nitrogen and oxygen atoms reside in the " para "-hydroxy of dopamine itself and its own intrinsic relation to DAT whereby that mutual hydroxyl functionality is mediated in both salicylmethylecgonine and dopamine in a similar manner.