N&PD Moderators: Skorpio | someguyontheinternet
Several esters of 1-(l -phenylcyclohexyl)-4-piperidinol(3)1, -(l -phenylcyclohexyl)-4-phenyl-4-piperidin(1o0l) and
its propionate (1l ),a nd 1-(l -phenylcyclohexyl)-4-phenylpiperidine(1 3) were prepared and characterized. The new
compounds, which are derived from phencyclidine, exerted analgesic activity in mice. The most potent is 10, which
is twice as active as morphine. The antinociceptive activity of 10, 11, and 13 could be well correlated with their
potency in the mouse vas deferens bioassay, and both were completely reversed by naloxone.
I liké Connie, nice one![]()
CHRISTA
1-phenyl-2-(hydroxyamino)propane
![]()
SAMMY
1-(2-methylthio-3,4,5-trimethoxyphenyl)-2-aminoethane
![]()
CONNIE
1-methyl-3-(indole-4-yl)-1-azacyclohex-2-ene
![]()
NURSE BETTY
2-methylamino-3-carbomethoxyindan
![]()
HYPER_ACTIVE
2-methylamino-1,3-dicarbomethoxyindan
![]()
HENRY
2-methylamino-1,3-dicarbomethotxy-5,6-methylenedioxyindan
![]()
JESSICA
2-ethylamino-1,3-dicarbomethoxy-5,6-methylenedioxyindan
![]()
HONEY BEAR
2-amino-1,3-dicarbomethoxy-4,7-dimethoxy-5,6-dimethylindan
Abstract
The serotonin (5-HT) receptor affinities and behavioral (discriminative stimulus) properties of a series of 4-substituted derivatives of 1-(2,5-dimethoxyphenyl)-2-aminopropanes (2,5-DMA) were investigated. The substituents at the 4-position included H, OMe, OEt, Me, Et, F, Br, I, and NO2. Substituent lipophilicities (pi values) of these functionalities appear to have a minimal effect on either 5-HT receptor affinity or behavioral activity. Those derivatives previously found to be most potent in human studies possess significant affinity for 5-HT receptors. Furthermore, when rats trained to discriminate (+/-)-1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) from saline were used, generalization was found to occur upon administration of the 4-substituted 2,5-DMA derivatives. Because a direct relationship exists between the ED50 values obtained from these discrimination studies and human hallucinogenic potencies, the discriminative stimulus paradigm, with DOM as a training drug, appears to be a useful tool for comparing the quantitative and qualitative (DOM-like) effects produced by certain hallucinogenic agents.