a(MESH:"3-(2,4-dimethoxybenzylidene)anabaseine")
In studies on SH-SY5Y cells and cultured rat hippocampal neurons, nicotine, acting through alpha7 nAChRs, results in the activation of ERK-1/2 pathways dependent upon calcium and protein kinase A (Dajas-Bailador et al., 2002b). In addition, the alpha7-specific agonist GTS-21 promotes ERK-1/2 phosphorylation, but not that of c-jun N-terminal kinase (JNK) or p38 (Ren et al., 2005). PubMed:19293145
In studies on SH-SY5Y cells and cultured rat hippocampal neurons, nicotine, acting through alpha7 nAChRs, results in the activation of ERK-1/2 pathways dependent upon calcium and protein kinase A (Dajas-Bailador et al., 2002b). In addition, the alpha7-specific agonist GTS-21 promotes ERK-1/2 phosphorylation, but not that of c-jun N-terminal kinase (JNK) or p38 (Ren et al., 2005). PubMed:19293145
In studies on SH-SY5Y cells and cultured rat hippocampal neurons, nicotine, acting through alpha7 nAChRs, results in the activation of ERK-1/2 pathways dependent upon calcium and protein kinase A (Dajas-Bailador et al., 2002b). In addition, the alpha7-specific agonist GTS-21 promotes ERK-1/2 phosphorylation, but not that of c-jun N-terminal kinase (JNK) or p38 (Ren et al., 2005). PubMed:19293145
In studies on SH-SY5Y cells and cultured rat hippocampal neurons, nicotine, acting through alpha7 nAChRs, results in the activation of ERK-1/2 pathways dependent upon calcium and protein kinase A (Dajas-Bailador et al., 2002b). In addition, the alpha7-specific agonist GTS-21 promotes ERK-1/2 phosphorylation, but not that of c-jun N-terminal kinase (JNK) or p38 (Ren et al., 2005). PubMed:19293145
Two partial agonists of alpha7 nAChRs, GTS-21 (also a strong alpha4beta2 antagonist) and MeM-3454 (also a strong 5-hydroxytryptamine type 3 receptor (5HT3) antagonist)149 (TABLe 1), further showed a procognitive action and, in preclinical studies, MeM-3454 enhanced episodic, spatial and working memory. PubMed:19721446
in a small Phase i clinical trial, GTS-21 improved episodic secondary memory tasks, including word recall, and picture and word recognition1 PubMed:19721446
As with nicotine, the weak alpha7 nAChR agonist GTS-21 is neuroprotective, specifically protecting against Abeta1–42-elicited neurotoxicity154. This effect is probably due to small, protracted increases in receptor-mediated Ca2+ influx. importantly, high concentrations of GTS-21 reduced cell survival, underlining the possible risk of over-stimulation152 PubMed:19721446
As with nicotine, the weak alpha7 nAChR agonist GTS-21 is neuroprotective, specifically protecting against Abeta1–42-elicited neurotoxicity154. This effect is probably due to small, protracted increases in receptor-mediated Ca2+ influx. importantly, high concentrations of GTS-21 reduced cell survival, underlining the possible risk of over-stimulation152 PubMed:19721446
As with nicotine, the weak alpha7 nAChR agonist GTS-21 is neuroprotective, specifically protecting against Abeta1–42-elicited neurotoxicity154. This effect is probably due to small, protracted increases in receptor-mediated Ca2+ influx. importantly, high concentrations of GTS-21 reduced cell survival, underlining the possible risk of over-stimulation152 PubMed:19721446
GTS-21, one of a series of compounds derived from anabaseine, an alkaloid found in marine worms, is a partial agonist of alpha7 nAChRs that improves memory-related behaviours in various paradigms and normalizes auditory gating186. it is the leading clinical candidate in the field of alpha7 nAChRs. PubMed:19721446
initially evaluated in normal subjects, GTS-21 was found to significantly improve attention and memory. in a second Phase i trial187, GTS-21 normalized P50 auditory gating in patients with schizophrenia. PubMed:19721446
GTS-21, one of a series of compounds derived from anabaseine, an alkaloid found in marine worms, is a partial agonist of alpha7 nAChRs that improves memory-related behaviours in various paradigms and normalizes auditory gating186. it is the leading clinical candidate in the field of alpha7 nAChRs. PubMed:19721446
initially evaluated in normal subjects, GTS-21 was found to significantly improve attention and memory. in a second Phase i trial187, GTS-21 normalized P50 auditory gating in patients with schizophrenia. PubMed:19721446
initially evaluated in normal subjects, GTS-21 was found to significantly improve attention and memory. in a second Phase i trial187, GTS-21 normalized P50 auditory gating in patients with schizophrenia. PubMed:19721446
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