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TCB2

CAS No. : 912342-28-0

MCE 站：TCB2

产品活性：TCB2 是 5-羟色胺 2A 受体 (5-HT_2A) 的激动剂.

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: The selective 5-HT_2A agonist TCB2 at 30 nM produces a marked shift to the right in the competition curve obtained with the 5-HT_1A receptor agonist ipsapirone from [³H]-8-OHDPAT binding sites in both areas of the brain. A significant increase in the mean K_i value is obtained with TCB2, demonstrating a reduction in the affinity of the high-affinity 5-HT_1A agonist binding sites by the 5-HT_2A agonist in both regions. In the case of hippocampus, there are also indications for antagonistic effects of ketanserin.

In Vivo: In an initial dose-response study, TCB2 (0.5, 1.0, ａnd 2.5 mg/kg) ａnd DOI (0.5, 1.0, 2.5, ａnd 5.0 mg/kg) induce head twitches in C57BL/6J mice in a dose-dependent manner compared to vehicle. Head twitches induced by TCB2 ａnd DOI are similar across the doses, with the exception that at the highest dose (5.0 mg/kg), TCB2 induces half as many head twitches as does DOI (p=0.021). Confirming 5-HT2A mediation of the head twitch response, in two separate studies, pretreatment with the selective 5-HT_2A antagonist MDL 11,939 (1.0 mg/kg) block head twitches induced by DOI (2.5 mg/kg) ａnd by TCB2 (2.5 mg/kg; p<0.0001). Compared to vehicle, corticosterone levels are increased following TCB2 (5.0 mg/kg, p=0.01; 10.0, p=0.012; with a trend following 2.5 mg/kg, p=0.079) ａnd DOI (10.0 mg/kg, p=0.035).

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