RU 24969

RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors; IC50 value:Target: 5-HT1A/1B agonistRU 24969 possesses preference for the purported 5-HT1B subtype of central 5-HT1 recognition site. The reported significant linear correlation between hypotensive activity following intravenous (i.v.) administration to anesthetized rats and affinity for the central 5-HT1 binding site could only be maintained by incorporation of the affinity of RU 24969 for its low and 8-OH-DPAT for its high affinity binding site [1]. The drug RU 24969 (10 mg/kg) inhibited the rate of synthesis of 5-HT in rat brain by about 50%. Pretreatment of rats with desmethylimipramine over a longer term or clenbuterol given acutely, treatments known to enhance the behavioural responses of rats to various other 5-HT agonists, did not alter the RU 24969-induced response [2]. RU 24969 (0.03-3.0mg/kg, s.c.) dose-dependently decreased water consumption in water deprived rats [3].

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

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

Research Areas >> Neurological Disease

[1]. Doods HN, et al. Differential selectivities of RU 24969 and 8-OH-DPAT for the purported 5-HT1A and 5-HT1B binding sites. Correlation between 5-HT1A affinity and hypotensive activity. Eur J Pharmacol. 1985 Jun 19;112(3):363-70.

[2]. Green AR, et al. The behavioural effects of RU 24969, a suggested 5-HT1 receptor agonist in rodents and the effect on the behaviour of treatment with antidepressants. Neuropharmacology. 1984 Jun;23(6):655-61.

[3]. Aronsen D, et al. RU 24969-produced adipsia and hyperlocomotion: Differential role of 5HT1A and 5HT1B receptor mechanisms. Pharmacol Biochem Behav. 2014 May 15;124C:1-4.

[4]. Cheetham SC, et al. Evidence that RU 24969-induced locomotor activity in C57/B1/6 mice is specifically mediated by the 5-HT1B receptor. Br J Pharmacol. 1993 Dec;110(4):1621-9.

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