DTG - CAS 97-39-2
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Sigma Receptor
DTG has been found to be a σ-receptor agonist and is useful in studies of its interaction with dopamine drug.
≥98% by HPLC
White Solid
1.Lack of cocaine-like discriminative-stimulus effects of σ-receptor agonists in rats.
Hiranita T1, Soto PL, Tanda G, Katz JL. Behav Pharmacol. 2011 Sep;22(5-6):525-30. doi: 10.1097/FBP.0b013e328349ab22.
Previous studies demonstrated the effectiveness of selective σ-receptor (σR) agonists [1,3-di-o-tolylguanidine (DTG), PRE-084] as reinforcers in rats trained to self-administer cocaine. Similar to cocaine, these drugs increased nucleus accumbens shell dopamine levels, and effects of DTG, but not PRE-084, on dopamine seemed to be mediated by σRs. In addition, σR antagonists blocked self-administration of σR agonists, but were inactive against reinforcing and neurochemical effects of cocaine. Thus, pharmacologically distinct mechanisms likely underlie the reinforcing and neurochemical effects of σR agonists and cocaine. This study further examined the cocaine-like effects of σR agonists in rats trained to discriminate injections of cocaine from saline to assess the similarity of their subjective effects. Standard dopamine-uptake inhibitors (WIN 35,428, methylphenidate), but neither σR agonist (PRE-084, DTG), produced full cocaine-like discriminative-stimulus effects.
2.N-substituted 8-aminopentacyclo[,6).0(3,10).0(5,9)]undecanes as σ receptor ligands with potential neuroprotective effects.
Banister SD1, Manoli M, Barron ML, Werry EL, Kassiou M. Bioorg Med Chem. 2013 Oct 1;21(19):6038-52. doi: 10.1016/j.bmc.2013.07.045. Epub 2013 Aug 6.
Several libraries of similarly N-substituted 8-aminopentacyclo[,6).0(3,10).0(5,9)]undecanes (9), N-methyl-8-aminopentacyclo[,6).0(3,10).0(5,9)]undecanes (14), and N-methyl-11-aminopentacyclo[,6).0(3,10).0(5,9)]undecan-8-ones (13) were synthesised and screened against a panel of CNS targets in order to develop structure-affinity relationships for cage-modified trishomocubane σ receptor ligands based on the N-substituted 4-azahexacyclo[,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ol (8) scaffold. In general, compared to the corresponding 4-azahexacyclo[,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols, compounds of type 9 were potent σ receptor ligands with low levels of subtype selectivity, while the corresponding N-methyl-8-aminopentacyclo[,6).0(3,10).0(5,9)]undecanes showed reduced affinity but greater selectivity for σ2 receptors. The N-methyl-11-aminopentacyclo[,6).0(3,10).0(5,9)]undecan-8-ones demonstrated the poorest σ receptor affinities, suggesting that 4-azahexacyclo[5.
3.Sigma-1 receptor agonists directly inhibit Nav1.2/1.4 channels.
Gao XF1, Yao JJ, He YL, Hu C, Mei YA. PLoS One. 2012;7(11):e49384. doi: 10.1371/journal.pone.0049384. Epub 2012 Nov 5.
(+)-SKF 10047 (N-allyl-normetazocine) is a prototypic and specific sigma-1 receptor agonist that has been used extensively to study the function of sigma-1 receptors. (+)-SKF 10047 inhibits K(+), Na(+) and Ca2+ channels via sigma-1 receptor activation. We found that (+)-SKF 10047 inhibited Na(V)1.2 and Na(V)1.4 channels independently of sigma-1 receptor activation. (+)-SKF 10047 equally inhibited Na(V)1.2/1.4 channel currents in HEK293T cells with abundant sigma-1 receptor expression and in COS-7 cells, which barely express sigma-1 receptors. The sigma-1 receptor antagonists BD 1063,BD 1047 and NE-100 did not block the inhibitory effects of (+)-SKF-10047. Blocking of the PKA, PKC and G-protein pathways did not affect (+)-SKF 10047 inhibition of Na(V)1.2 channel currents. The sigma-1 receptor agonists Dextromethorphan (DM) and 1,3-di-o-tolyl-guanidine (DTG) also inhibited Na(V)1.2 currents through a sigma-1 receptor-independent pathway. The (+)-SKF 10047 inhibition of Na(V)1.
4.Live imaging reveals a new role for the sigma-1 (σ1) receptor in allowing microglia to leave brain injuries.
Moritz C1, Berardi F2, Abate C3, Peri F4. Neurosci Lett. 2015 Mar 30;591:13-8. doi: 10.1016/j.neulet.2015.02.004. Epub 2015 Feb 7.
Microglial cells are responsible for clearing and maintaining the central nervous system (CNS) microenvironment. Upon brain damage, they move toward injuries to clear the area by engulfing dying neurons. However, in the context of many neurological disorders chronic microglial responses are responsible for neurodegeneration. Therefore, it is important to understand how these cells can be "switched-off" and regain their ramified state. Current research suggests that microglial inflammatory responses can be inhibited by sigma (σ) receptor activation. Here, we take advantage of the optical transparency of the zebrafish embryo to study the role of σ1 receptor in microglia in an intact living brain. By combining chemical approaches with real time imaging we found that treatment with PB190, a σ1 agonist, blocks microglial migration toward injuries leaving cellular baseline motility and the engulfment of apoptotic neurons unaffected. Most importantly, by taking a reverse genetic approach, we discovered that the role of σ1in vivo is to "switch-off" microglia after they responded to an injury allowing for these cells to leave the site of damage.
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CAS 97-39-2 DTG

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