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439 results
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Page 1
Synthesis of (-)-Picrotoxinin by Late-Stage Strong Bond Activation.
Crossley SWM, Tong G, Lambrecht MJ, Burdge HE, Shenvi RA. Crossley SWM, et al. J Am Chem Soc. 2020 Jul 1;142(26):11376-11381. doi: 10.1021/jacs.0c05042. Epub 2020 Jun 23. J Am Chem Soc. 2020. PMID: 32573211 Free PMC article.
We report a concise, stereocontrolled synthesis of the neurotoxic sesquiterpenoid (-)-picrotoxinin (1, PXN). The brevity of the route is due to regio- and stereoselective formation of the [4.3.0] bicyclic core by incorporation of a symmetrizing geminal dimethyl group at C5 …
We report a concise, stereocontrolled synthesis of the neurotoxic sesquiterpenoid (-)-picrotoxinin (1, PXN). The brevity of the route …
Picrotoxinin and related substances.
Porter LA. Porter LA. Chem Rev. 1967 Aug;67(4):441-64. doi: 10.1021/cr60248a004. Chem Rev. 1967. PMID: 4859924 Review. No abstract available.
Comparison of the toxicokinetics of the convulsants picrotoxinin and tetramethylenedisulfotetramine (TETS) in mice.
Pressly B, Vasylieva N, Barnych B, Singh V, Singh L, Bruun DA, Hwang SH, Chen YJ, Fettinger JC, Johnnides S, Lein PJ, Yang J, Hammock BD, Wulff H. Pressly B, et al. Arch Toxicol. 2020 Jun;94(6):1995-2007. doi: 10.1007/s00204-020-02728-z. Epub 2020 Apr 1. Arch Toxicol. 2020. PMID: 32239239 Free PMC article.
Here, we directly compared the toxicokinetics of the two compounds following intraperitoneal administration in mice. Using LC/MS analysis we found that picrotoxinin, the active component of picrotoxin, hydrolyses quickly into picrotoxic acid, has a short in vivo half-life, …
Here, we directly compared the toxicokinetics of the two compounds following intraperitoneal administration in mice. Using LC/MS analysis we …
Mechanisms for picrotoxinin and picrotin blocks of alpha2 homomeric glycine receptors.
Wang DS, Buckinx R, Lecorronc H, Mangin JM, Rigo JM, Legendre P. Wang DS, et al. J Biol Chem. 2007 Jun 1;282(22):16016-35. doi: 10.1074/jbc.M701502200. Epub 2007 Apr 3. J Biol Chem. 2007. PMID: 17405877 Free article.
Although both picrotoxinin and picrotin inhibited glycine-evoked outside-out currents, picrotin had a 30 times higher IC50 than picrotoxinin. ...Our data indicate that picrotoxinin and picrotin are not equivalent in blocking alpha2 homomeric GlyR....
Although both picrotoxinin and picrotin inhibited glycine-evoked outside-out currents, picrotin had a 30 times higher IC50 than pi
Revision of the Unstable Picrotoxinin Hydrolysis Product.
Tong G, Shenvi RA. Tong G, et al. Angew Chem Int Ed Engl. 2021 Aug 23;60(35):19113-19116. doi: 10.1002/anie.202107785. Epub 2021 Jul 20. Angew Chem Int Ed Engl. 2021. PMID: 34236745
The plant metabolite picrotoxinin (PXN) is a widely used tool in neuroscience for the identification of GABAergic signaling. ...
The plant metabolite picrotoxinin (PXN) is a widely used tool in neuroscience for the identification of GABAergic signaling. ...
The binding mode of picrotoxinin in GABA(A-rho) receptors: Insight into the subunit's selectivity in the transmembrane domain.
Naffaa MM, Samad A. Naffaa MM, et al. Comput Biol Chem. 2016 Oct;64:202-209. doi: 10.1016/j.compbiolchem.2016.07.003. Epub 2016 Jul 7. Comput Biol Chem. 2016. PMID: 27423910
The channel blocker picrotoxinin has been studied with GABA(A-rho1) and GABA(A-rho2) homology models based on the GluCl crystal structure. Picrotoxinin is tenfold more potent for GABA(A-rho2) than for GABA(A-rho1) homomeric channels. ...
The channel blocker picrotoxinin has been studied with GABA(A-rho1) and GABA(A-rho2) homology models based on the GluCl crystal struc …
Effects of bilobalide, ginkgolide B and picrotoxinin on GABA(A) receptor modulation by structurally diverse positive modulators.
Ng CC, Duke RK, Hinton T, Johnston GAR. Ng CC, et al. Eur J Pharmacol. 2017 Jul 5;806:83-90. doi: 10.1016/j.ejphar.2017.04.019. Epub 2017 Apr 15. Eur J Pharmacol. 2017. PMID: 28416372
Like picrotoxinin, bilobalide and ginkgolide B, active constituents of Ginkgo biloba, have been shown to negatively modulate the action of GABA at alpha(1)beta(2)gamma(2L) GABA(A) receptors. However, unlike picrotoxinin, bilobalide and ginkgolide B are not known to …
Like picrotoxinin, bilobalide and ginkgolide B, active constituents of Ginkgo biloba, have been shown to negatively modulate the acti …
Studies on the mechanism of action of picrotoxinin and other convulsants at the crustacean muscle GABA receptor.
Smart TG, Constanti A. Smart TG, et al. Proc R Soc Lond B Biol Sci. 1986 Mar 22;227(1247):191-216. doi: 10.1098/rspb.1986.0019. Proc R Soc Lond B Biol Sci. 1986. PMID: 26151987
The actions of picrotoxinin, bicuculline and penicillin-G were investigated on the GABA-receptor system of lobster muscle by using intracellular recording. ...It is suggested that picrotoxinin and bicuculline may antagonize GABA responses by stabilizing the closed f …
The actions of picrotoxinin, bicuculline and penicillin-G were investigated on the GABA-receptor system of lobster muscle by using in …
The picrotoxinin binding site and its relationship to the GABA receptor complex.
White WF, Snodgrass SR, Dichter MA. White WF, et al. J Neurochem. 1985 Mar;44(3):812-7. doi: 10.1111/j.1471-4159.1985.tb12888.x. J Neurochem. 1985. PMID: 2983020
The binding characteristics of [3H] alpha-dihydropicrotoxinin to the picrotoxinin binding site were investigated in membrane preparations of adult rat forebrain and living cultures of rat cerebral cortex. ...The Hill coefficients for these actions were reciprocal, suggesti …
The binding characteristics of [3H] alpha-dihydropicrotoxinin to the picrotoxinin binding site were investigated in membrane preparat …
439 results