| http://purl.uniprot.org/citations/12065717 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/12065717 | http://www.w3.org/2000/01/rdf-schema#comment | "The plant alkaloid methyllycaconitine (MLA) is considered to be a selective antagonist of the alpha7 subtype of neuronal nicotinic acetylcholine receptor (nAChR). However, 50 nM MLA partially inhibited (by 16%) [(3)H]dopamine release from rat striatal synaptosomes stimulated with 10 microM nicotine. Other alpha7-selective antagonists had no effect. Similarly, MLA (50 nM) inhibited [(3)H]dopamine release evoked by the partial agonist (2-chloro-5-pyridyl)-9-azabicyclo[4.2.1]non-2-ene (UB-165) (0.2 microM) by 37%. In both cases, inhibition by MLA was surmountable with higher agonist concentrations, indicative of a competitive interaction. At least two subtypes of presynaptic nAChR can modulate dopamine release in the striatum, and these nAChR are distinguished by their differential sensitivity to alpha-conotoxin-MII (alpha-CTx-MII). MLA was not additive with a maximally effective concentration of alpha-CTx-MII (100 nM) in inhibiting [(3)H]dopamine release elicited by 10 microM nicotine or 0.2 microM UB-165, suggesting that both toxins act at the same site. This was confirmed in quantitative binding assays with (125)I-alpha-CTx-MII, which displayed saturable specific binding to rat striatum and nucleus accumbens with B(max) values of 9.8 and 16.5 fmol/mg of protein, and K(d) values of 0.63 and 0.83 nM, respectively. MLA fully inhibited (125)I-alpha-CTx-MII binding to striatum and nucleus accumbens with a K(i) value of 33 nM, consistent with the potency observed in the functional assays. We speculate that MLA and alpha-CTx-MII interact with a presynaptic nAChR of subunit composition alpha3/alpha6beta2beta3* on dopamine neurons. The use of MLA as an alpha7-selective antagonist should be exercised with caution, especially in studies of nAChR in basal ganglia."xsd:string |
| http://purl.uniprot.org/citations/12065717 | http://purl.org/dc/terms/identifier | "doi:10.1124/jpet.302.1.197"xsd:string |
| http://purl.uniprot.org/citations/12065717 | http://purl.uniprot.org/core/author | "Collins A.C."xsd:string |
| http://purl.uniprot.org/citations/12065717 | http://purl.uniprot.org/core/author | "McIntosh J.M."xsd:string |
| http://purl.uniprot.org/citations/12065717 | http://purl.uniprot.org/core/author | "Wonnacott S."xsd:string |
| http://purl.uniprot.org/citations/12065717 | http://purl.uniprot.org/core/author | "Whiteaker P."xsd:string |
| http://purl.uniprot.org/citations/12065717 | http://purl.uniprot.org/core/author | "Marks M."xsd:string |
| http://purl.uniprot.org/citations/12065717 | http://purl.uniprot.org/core/author | "Mogg A.J."xsd:string |
| http://purl.uniprot.org/citations/12065717 | http://purl.uniprot.org/core/date | "2002"xsd:gYear |
| http://purl.uniprot.org/citations/12065717 | http://purl.uniprot.org/core/name | "J Pharmacol Exp Ther"xsd:string |
| http://purl.uniprot.org/citations/12065717 | http://purl.uniprot.org/core/pages | "197-204"xsd:string |
| http://purl.uniprot.org/citations/12065717 | http://purl.uniprot.org/core/title | "Methyllycaconitine is a potent antagonist of alpha-conotoxin-MII-sensitive presynaptic nicotinic acetylcholine receptors in rat striatum."xsd:string |
| http://purl.uniprot.org/citations/12065717 | http://purl.uniprot.org/core/volume | "302"xsd:string |
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