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Structure-based design, synthesis, and biochemical and pharmacological characterization of novel salvinorin A analogues as active state probes of the kappa-opioid receptor.

Yan F, Bikbulatov RV, Mocanu V, Dicheva N, Parker CE, Wetsel WC, Mosier PD, Westkaemper RB, Allen JA, Zjawiony JK, Roth BL.

Biochemistry. 2009 Jul 28;48(29):6898-908. doi: 10.1021/bi900605n.


Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.

Polepally PR, Huben K, Vardy E, Setola V, Mosier PD, Roth BL, Zjawiony JK.

Eur J Med Chem. 2014 Oct 6;85:818-29. doi: 10.1016/j.ejmech.2014.07.077. Epub 2014 Aug 23.


Salvinorin A: the "magic mint" hallucinogen finds a molecular target in the kappa opioid receptor.

Sheffler DJ, Roth BL.

Trends Pharmacol Sci. 2003 Mar;24(3):107-9. Review.


Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo.

Wang Y, Tang K, Inan S, Siebert D, Holzgrabe U, Lee DY, Huang P, Li JG, Cowan A, Liu-Chen LY.

J Pharmacol Exp Ther. 2005 Jan;312(1):220-30. Epub 2004 Sep 21.


Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to kappa-opioid receptors.

Yan F, Mosier PD, Westkaemper RB, Stewart J, Zjawiony JK, Vortherms TA, Sheffler DJ, Roth BL.

Biochemistry. 2005 Jun 21;44(24):8643-51.


Kappa-opioid receptor-selective dicarboxylic ester-derived salvinorin A ligands.

Polepally PR, White K, Vardy E, Roth BL, Ferreira D, Zjawiony JK.

Bioorg Med Chem Lett. 2013 May 15;23(10):2860-2. doi: 10.1016/j.bmcl.2013.03.111. Epub 2013 Apr 4.


Salvinorin A: a novel and highly selective kappa-opioid receptor agonist.

Yan F, Roth BL.

Life Sci. 2004 Oct 15;75(22):2615-9. Review.


Kappa opioid mediation of cannabinoid effects of the potent hallucinogen, salvinorin A, in rodents.

Walentiny DM, Vann RE, Warner JA, King LS, Seltzman HH, Navarro HA, Twine CE Jr, Thomas BF, Gilliam AF, Gilmour BP, Carroll FI, Wiley JL.

Psychopharmacology (Berl). 2010 Jun;210(2):275-84. doi: 10.1007/s00213-010-1827-6. Epub 2010 Mar 31.


Immediate and Persistent Effects of Salvinorin A on the Kappa Opioid Receptor in Rodents, Monitored In Vivo with PET.

Placzek MS, Van de Bittner GC, Wey HY, Lukas SE, Hooker JM.

Neuropsychopharmacology. 2015 Dec;40(13):2865-72. doi: 10.1038/npp.2015.159. Epub 2015 Jun 10.


Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.

Kane BE, McCurdy CR, Ferguson DM.

J Med Chem. 2008 Mar 27;51(6):1824-30. doi: 10.1021/jm701040v. Epub 2008 Feb 23.


Synthesis and κ-opioid receptor activity of furan-substituted salvinorin A analogues.

Riley AP, Groer CE, Young D, Ewald AW, Kivell BM, Prisinzano TE.

J Med Chem. 2014 Dec 26;57(24):10464-75. doi: 10.1021/jm501521d. Epub 2014 Dec 9.


Salvinorin A, an active component of the hallucinogenic sage salvia divinorum is a highly efficacious kappa-opioid receptor agonist: structural and functional considerations.

Chavkin C, Sud S, Jin W, Stewart J, Zjawiony JK, Siebert DJ, Toth BA, Hufeisen SJ, Roth BL.

J Pharmacol Exp Ther. 2004 Mar;308(3):1197-203. Epub 2004 Jan 8.


Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues.

Béguin C, Potuzak J, Xu W, Liu-Chen LY, Streicher JM, Groer CE, Bohn LM, Carlezon WA Jr, Cohen BM.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1023-6. doi: 10.1016/j.bmcl.2011.11.128. Epub 2011 Dec 7.


Antinociceptive and hypothermic effects of Salvinorin A are abolished in a novel strain of kappa-opioid receptor-1 knockout mice.

Ansonoff MA, Zhang J, Czyzyk T, Rothman RB, Stewart J, Xu H, Zjwiony J, Siebert DJ, Yang F, Roth BL, Pintar JE.

J Pharmacol Exp Ther. 2006 Aug;318(2):641-8. Epub 2006 May 3.


Kappa-opioid receptor-mediated effects of the plant-derived hallucinogen, salvinorin A, on inverted screen performance in the mouse.

Fantegrossi WE, Kugle KM, Valdes LJ 3rd, Koreeda M, Woods JH.

Behav Pharmacol. 2005 Dec;16(8):627-33.


Opioid receptor probes derived from cycloaddition of the hallucinogen natural product salvinorin A.

Lozama A, Cunningham CW, Caspers MJ, Douglas JT, Dersch CM, Rothman RB, Prisinzano TE.

J Nat Prod. 2011 Apr 25;74(4):718-26. doi: 10.1021/np1007872. Epub 2011 Feb 21.


Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids.

Fichna J, Lewellyn K, Yan F, Roth BL, Zjawiony JK.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):160-3. doi: 10.1016/j.bmcl.2010.11.046. Epub 2010 Nov 11.


Neuropharmacology of the naturally occurring kappa-opioid hallucinogen salvinorin A.

Cunningham CW, Rothman RB, Prisinzano TE.

Pharmacol Rev. 2011 Jun;63(2):316-47. doi: 10.1124/pr.110.003244. Epub 2011 Mar 28. Review.


Chemotype-selective modes of action of κ-opioid receptor agonists.

Vardy E, Mosier PD, Frankowski KJ, Wu H, Katritch V, Westkaemper RB, Aubé J, Stevens RC, Roth BL.

J Biol Chem. 2013 Nov 29;288(48):34470-83. doi: 10.1074/jbc.M113.515668. Epub 2013 Oct 11.

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