Journal of Pharmaceutical Sciences
August 23, 2012
Malcolm Rowland
51 citations
Ultrasensitive analytical methodologies have now made possible the ability to characterize the pharmacokinetics (PK) of compounds following administration to humans of a minute, subpharmacologic dose, a microdose. This has the potential to provide pre-IND information to help in early candidate selection, but only if such information is reasonably predictive of PK at pharmacologic doses. The...
Journal of Pharmaceutical Sciences
December 1, 2009
Nicolas Tournier, Pascal André, Sandy Blondeel et al.
14 citations
The (99m)Tc-tricarbonyl core may be used as an ideal tool for gamma-labeling ligands in noninvasive SPECT imaging. However, most (99m)Tc-tricarbonyl-labeled agents have difficulty crossing the blood-brain barrier (BBB). We radiolabeled the neuroactive indole ibogaine with (99m)Tc-tricarbonyl and measured its transport into the mouse brain by in situ brain perfusion. We measured the interactions...
Journal of Pharmaceutical Sciences
March 1, 1983
Michal W. Majchrzak, A Kotełko, Roman Guryn et al.
5 citations
Structural juxtaposition of the 3,4,5-trimethoxyphenyl group in the same molecule with a piperazine or homopiperazine ring has been realized in a series of mescaline analogues (I-IV) as part of an investigation into the pharmacological properties of the seven-membered perhydro-1,4-diazepines (homopiperazines). The analogous six-membered piperazines were synthesized and tested as reference...
Journal of Pharmaceutical Sciences
1980
C. Van Peteghem, A. Heyndrickx, W. Van Zele
11 citations
A GLC-mass spectral analysis with a deuterated internal standard was developed to measure plasma mescaline concentrations after intravenous administration to rabbits. The drug and the internal standard were extracted with benzene, derivatized with trifluoroacetic acid anhydride, and chromatographed on 2.5% QF-1 with mass fragmentographic detection. The detection limit is 5 ng/ml of plasma. The...
Journal of Pharmaceutical Sciences
July 1, 1979
Richard A Glennon, Lemont B. Kier, Alexander T. Shulgin
29 citations
The hallucinogenic (psychotomimetic) potency of 10 mescaline analogs was examined by molecular connectivity analysis. Potencies could be described by a two-term relating equation, which explained 94% of the variance in activity, on the basis of structural variation, 2,5-Dimethoxy substitution as well as the nature of the 4-position substituent played an important role in determining...
Journal of Pharmaceutical Sciences
July 1, 1977
Peter K. S. Siegl, Raymond F. Orzechowski
2 citations
Mescaline, in concentrations of 5 x 10(-4) and 1 x 10(-3) M, produced negative chronotropic and positive inotropic responses in isolated, spontaneously beating rat atria. In tissues driven at a constant rate, the inotropic response was diminished greatly, indicating that the increment in the force of contraction was secondary to the reduction in rate. These chronotropic and inotropic responses...
Journal of Pharmaceutical Sciences
May 1, 1977
David B. Repke, Dale Thomas Leslie, Daniel Mandell et al.
31 citations
With the combined technique of GLC-mass spectrometry, psilocin and psilocybin, two hallucinogenic indoles, were analyzed as their trimethylsilyl derivatives. The method was applied to these two components in an extract of Psilocybe cubensis (Earle) Sing.
Journal of Pharmaceutical Sciences
October 1, 1976
F. Jun. Desantis, Karl A. Nieforth
4 citations
1-[2-(3,4,5-Trimethoxyphenyl)ethyl]-3-pyrroline, 2-(3,4,5-trimethoxybenzyl)-1,2,3,6-tetrahydropyridine, N-n-propylmescaline, N-cyclopropylmethylmescaline, and N-allylmescaline were synthesized as potential mescaline antagonists. The ability of these compounds to antagonize mescaline-induced disruption of swim behavior is also given.
Journal of Pharmaceutical Sciences
December 1, 1975
Robert J. Wolters, Ansuman Bej, N. S. Tanner
5 citations
The synthesis of methyl-2-(3,4,5-trimethoxyphenyl)-2-(2-piperidyl) acetate is described. In addition, preliminary pharmacological data comparing the compound with mescaline are given.