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CAS No. :
MCE 国际站:RTI-13951-33 hydrochloride
产品活性:RTI-13951-33 hydrochloride 是一种有效、选择性、可透过血脑屏障的 GPR88 激动剂,在 GPR88 cAMP 功能性实验中,EC50 值为 25 nM。RTI-13951-33 hydrochloride 可以减少大鼠酒精强化和摄取行为。
研究领域:GPCR/G Protein
作用靶点:GPR88
In Vitro: RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 elevates [35S]-GTPγS binding (EC50, 535 nM) in mouse striatal membranes but not in membranes from GPR88 KO mice.
RTI-13951-33 has weak affinities at kappa opioid receptor (KOR; Ki, 2.29 μM), vesicular monoamine transporter (VMAT; Ki, 4.23 μM), and moderate affinity at serotonin transporter (SERT; Ki, 0.75 μM), however, RTI-13951-33 poorly inhibits SERT (IC50, 25.1±2.7 μM).
In Vivo: RTI-13951-33 (10 and 20 mg/kg, i.p.) dose-dependently decreases alcohol lever responses in a rat model of alcohol self-administration.
RTI-13951-33 (10 mg/kg, i.p.) has sufficient brain penetration, with t1/2 of 48 min and 87 min in rat plasma and brain.
相关产品:Bioactive Compound Library Plus | GPCR/G Protein Compound Library | CNS-Penetrant Compound Library | Targeted Diversity Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | RTI-13951-33 | (1R,2R)-2-PCCA hydrochloride
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货号: HY-112612A
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