RU 24969 hemisuccinate

Names

[ Name ]:
RU 24969 hemisuccinate

[Synonym ]:
5-Methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole succinate (2:1)
5-methoxy-3(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole succinate
1H-Indole, 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-, butanedioate (2:1)
Succinic acid - 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole (1:2)
5-METHOXY-3-(1,2,5,6-TETRAHYDRO-4-PYRIDINYL)-1H-INDOLE HEMISUCCINATE

Biological Activity

[Description]:

RU 24969 succinate is a 5-HT receptor agonist with Ki values of 0.38 and 2.5 nM for 5-HT1B and 5-HT1A, respectively. RU 24969 decreases fluid consumption and increases forward locomotion. RU 24969 succinate can be used for the research of neurological disease[1][2][3][4].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

Ki: 0.38 nM (5-HT1B), 2.5 nM (5-HT1A)[3]

[In Vitro]

RU 24969 succinate (30 nM-1 μM) 抑制 K+ 诱发的氚外排，在 1 μM 浓度下 pD2 为 7.45[1]。

[In Vivo]

RU 24969 succinate (1 和 3 mg/kg；皮下注射，1 次) 增强可卡因诱导产生的作用[2]。 RU 24969 succinate (0.03-3.0 mg/kg；皮下注射，1 次) 剂量依赖性地减少水剥夺大鼠的水消耗[4]。 Animal Model: Male Wistar rats with cocaine injection[2] Dosage: 1 and 3 mg/kg Administration: Subcutaneous injection; 1 and 3 mg/kg, once Result: Increased cocaine-induced elevation of nucleus accumbens (NAcc) dopamine DA levels and reduction of ventral tegmental area (VTA) GABA levels.

[References]

[1]. Middlemiss DN. The putative 5-HT1 receptor agonist, RU 24969, inhibits the efflux of 5-hydroxytryptamine from rat frontal cortex slices by stimulation of the 5-HT autoreceptor. J Pharm Pharmacol. 1985 Jun;37(6):434-7.

[2]. Parsons LH, et al. RU 24969, a 5-HT1B/1A receptor agonist, potentiates cocaine-induced increases in nucleus accumbens dopamine. Synapse. 1999 May;32(2):132-5.

[3]. Peroutka SJ. Pharmacological differentiation and characterization of 5-HT1A, 5-HT1B, and 5-HT1C binding sites in rat frontal cortex. J Neurochem. 1986 Aug;47(2):529-40.

[4]. Aronsen D, et al. RU 24969-produced adipsia and hyperlocomotion: differential role of 5HT 1A and 5HT 1B receptor mechanisms. Pharmacol Biochem Behav. 2014 Sep;124:1-4.