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Glossary of Terms Used in Medicinal Chemistry
- B. S. Fulton
- 26 September 2014
Modulation of prepulse inhibition through both M1 and M4 muscarinic receptors in mice
- Morgane Thomsen, J. Wess, B. S. Fulton, A. Fink-Jensen, S. B. Caine
- Psychology, BiologyPsychopharmacology
- 1 February 2010
The results do not support a role of M1/M4 receptors in mediating antipsychotic-like effects of clozapine and haloperidol, but suggest that xanomeline exerts antippsychotic- like effects mainly through M4 receptor stimulation, while stimulation of non-M1/ M4 subtypes may also have antipsychosis potential.
Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice
Attenuation of the cocaine stimulus by VU0357017 depended upon M1 receptors, and full effects of xanomeline depended upon both M1 and M4 receptors, therefore M1-selective agonists and mixed M1/M4 agonists may be promising leads for developing medications that block cocaine’s effects.
Mechanism of action of aromatic amines that short-circuit the visual cycle.
The "short-circuit" hypothesis is investigated more fully and Numerous phenetidine-like molecules are assayed for their ability to inhibit rhodopsin formation and 11-cis-retinyl palmitate formation in the living frog eye.
Attenuation of Cocaine's Reinforcing and Discriminative Stimulus Effects via Muscarinic M1 Acetylcholine Receptor Stimulation
- Morgane Thomsen, P. Conn, S. B. Caine
- Biology, PsychologyJournal of Pharmacology and Experimental…
- 1 March 2010
The data suggest that central M1 receptor activation attenuates cocaine's abuse-related effects, whereas non-M1/M4 receptors probably contribute to undesirable effects of muscarinic stimulation.
Acute and chronic effects of the M1/M4-preferring muscarinic agonist xanomeline on cocaine vs. food choice in rats
The notion that chronic muscarinic receptor stimulation can reduce cocaine self-administration in mice is supported and xanomeline's potential for promoting abstinence from cocaine in humans is mixed, suggesting clinical usefulness may be limited.
Aliphatic acyl transfer in the Baker-Venkataraman reaction
Synthese de β-dicetones (sous la forme cetoenol) par reaction de derives d'hydroxy-2' acetophenones avec des chlorures d'acyle en presence de NaH dans THF
Biosynthesis of 11-cis-retinoids and retinyl esters by bovine pigment epithelium membranes.
It is shown that, in the bovine system, the activity resides exclusively in the membranes of the pigment epithelium, and diverse chemical reagents inhibit both ester synthetase and isomerase activities in a roughly parallel fashion, suggesting a possible functional linkage between the two activities.
Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.
- M. Decker, B. S. Fulton, Bin Zhang, Brian I. Knapp, J. Bidlack, J. Neumeyer
- Biology, ChemistryJournal of medicinal chemistry
- 10 December 2009
Bivalent morphinan compounds containing ester linkers were synthesized and their binding affinities at the mu, delta, and kappa opioid receptors determined, and 4a and 4b were partial agonists at the kappa and micro receptors in the [(35)S]GTPgammaS binding assay.
In Vivo Characterization of (−)(−)MCL-144 and (+)(−)MCL-193: Isomeric, Bivalent Ligands with Mu/Kappa Agonist Properties
- Jennifer L. Mathews, B. S. Fulton, S. Negus, J. Neumeyer, J. Bidlack
- Biology, ChemistryNeurochemical Research
- 5 June 2008
This study addressed whether two isomeric bivalent ligands would have pharmacological differences after central administration, in vivo, and demonstrated that having two active pharmacophores separated by a 10-carbon spacer group did not increase the antinociceptive efficacy of the compound.