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Chemical Compound Review

AC1MHFI6     butanedioic acid; 5-methoxy-3-(1,2,3,6...

Synonyms: LS-83244, HMS3267A17, 66611-27-6, MolPort-003-983-676
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Disease relevance of RU 24969

  • In rats the hypothermia induced by 8-OH-DPAT was partially antagonised by TVX Q 7821 while the behavioural "serotonin syndrome" induced by 8-OH-DPAT (a possible post-synaptic 5-HT1B-mediated effect) was unaffected by TVX Q 7821 as was the locomotion induced by RU 24969 [1].
  • RU 24969-induced emesis in the cat: 5-HT1 sites other than 5-HT1A, 5-HT1B or 5-HT1C implicated [2].
  • Unlike in the rat, RU 24969 did not elicit hypotension in the pig [3].
  • The 5-HT2A/2C receptor agonist DOI (10-20 nmol/0.5 microliter) significantly reduced NPY overeating while the 5-HT1A/1B receptor agonist RU 24969 (3.5-14 nmol/0.5 microliter) and the 5-HT1B/2C receptor agonist mCPP (5-20 nmol/0.5 microliter) had no such effect [4].
  • The mixed 5-HT-1A and 5-HT-1B agonist RU 24969 reversed catalepsy only at the highest dose tested [5].

Psychiatry related information on RU 24969


High impact information on RU 24969

  • Self-administration behavior was not maintained when either RU 24969 or CP 94,253 was substituted for cocaine, indicating that these 5-HT1B agonists do not produce significant reinforcing effects alone [9].
  • In the absence of VIP, cAMP formation could be stimulated through a 5-HT receptor, but the specific 5-HT1A agonists, 8-OH-DPAT and RU 24969 did not stimulate cAMP production [10].
  • RU 24969 significantly reduced Bmax 23 to 63% in cortex, hippocampus, striatum, brainstem, and spinal cord without a change in Ka except for a 1.7-fold increase in cortex and spinal cord [11].
  • Using the Behavioral Pattern Monitor (BPM), the profile of behavioral effects of a 5-HT1B agonist, 5-methoxy-3(1,2,3,6)tetrahydropyridin-4yl)-1H-indole (RU 24969), was compared to that previously described for MDMA and related indirect 5-HT agonists [12].
  • The ability of RU 24969 (0.5, 1, 5, and 10 mg/kg, ip) to elevate PRL secretion was not inhibited by pretreatment with p-chlorophenylalanine, suggesting that RU 24969 stimulates PRL secretion only through activation of postsynaptic 5-HT receptors [13].

Chemical compound and disease context of RU 24969


Biological context of RU 24969

  • Some behavioural and biochemical consequences of the administration of RU 24969 (5-methoxy-3(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole), a drug which has been shown to be a potent displacing agent at the 5-HT1 binding site, have been studied in mice and rats [7].
  • The results support the view that RU-24969 stimulates a 5-HT1 receptor that is involved in the autoregulation of 5-HT release and metabolism [16].
  • When animals were restrained from moving, RU 24969 dose-dependently reduced body temperature, an effect that may also be associated with activation of the 5-HT1A recognition site [17].
  • In contrast to these results medial hypothalamic infusion of TFMPP or RU 24969 (12.5-50 nmol) failed to affect food intake in any of the 3 tests [18].
  • Additionally, this study quantitatively examined the effect of quinpirole pretreatment on the ability of RU-24969 to induce both locomotor hyperactivity and striatal immediate early gene expression [19].

Anatomical context of RU 24969

  • This residual 49% of [3H]5-HT binding to spinal cord synaptosomes observed in the presence of 100 nM 8-OH-DPAT and 10 nM RU 24969 (subsequently referred to as "5-HT1S") displayed high affinity and saturability (KD = 4.7 nM) in association/dissociation and saturation experiments [20].
  • The 5-HT1A/1B receptor agonist RU 24969 was 10 times more potent at inhibiting [3H]5-HT overflow in the rat frontal cortex than in the human neocortex [21].
  • The effect of RU 24969 infusion (1 microM) was attenuated by concurrent infusion of metitepine (10 microM) into the hippocampus [22].
  • RU-24969 2.5 and 5 mg/kg had no effect on DA synthesis in the striatum, while 5.0 mg/kg significantly increased it in the nucleus accumbens [23].
  • In some brain areas such as the globus pallidus and dorsal subiculum, binding of ICYP was blocked with high affinity by some serotoninergic ligands, RU-24969 and serotonin, but not by lysergic acid diethylamide and 8-hydroxy-2-(N,N-di-n-propylamino)tetralin [24].

Associations of RU 24969 with other chemical compounds

  • Although the effects of MDMA on 5-HT1B receptors are secondary to its ability to release presynaptic 5-HT, the activation produced by RU 24969 appears to be a consequence of its direct agonist effects [12].
  • Ipsapirone (0.25-5.0 mg/kg) increased OTR and at 1.0 mg/kg antagonised the anxiogenic action of 8-OH-D-PAT, RU 24969 and BAY R 1531 [25].
  • The non-selective 5-HT antagonist metergoline prevented the RU-24969-induced decrease in 5-HT release and metabolism in vivo while the 5-HT2 receptor antagonist R-55669 (ritanserin) did not [16].
  • 3. The affinities of 8-OH-DPAT, RU 24969 and methysergide determined against [3H]-idazoxan binding to the cortex and hippocampus correlate significantly with the binding site displaying low affinity for prazosin and previously designated alpha 2A [26].
  • The relative potency, 8-hydroxy-2-(di-n-propylamino)tetra lin (8-OH-DPAT) much greater than 5-methoxy-N,N-dimethyltryptamine (5-MeODMT) greater than or equal to 5-methoxy-3(tetrahydropyridin-4-yl)1H-indole (RU 24969), was unrelated to the occurrence of wet dog shakes and suggests that 5-HT1 rather than 5-HT2 receptors may be involved [27].

Gene context of RU 24969

  • RU 24969, a tetrahydropyridoindole derivative that is a potent 5-HT1A and 5-HT1B agonist was also inactive, whereas RU 28253, another member of this series, could stimulate cAMP production [28].
  • The 5-HT1A/1b agonist, RU 24969 (0.03-0.3 mg/kg), reduced chain lengths [29].
  • Inasmuch as 5-HT2 receptors mediate the serotonergic stimulation of renin secretion, we examined the ability of two selective 5-HT2 antagonists, ritanserin and LY53857, to inhibit the neuroendocrine effects of RU 24969 [30].
  • Because the 5-HT1B agonist RU 24969 disrupts PPI and stimulates locomotor behavior in rats, it was predicted that the 5-HT1D agonist, SDZ 219-964, would demonstrate a similar behavioral profile in guinea pigs [31].
  • The cardiovascular effects of RU 24969 were antagonized neither by MDL 72222 nor by ICS 205-930 (5-HT3 receptor antagonists) [32].

Analytical, diagnostic and therapeutic context of RU 24969

  • The pharmacological responses to intraperitoneal injection of the serotonin (5-HT) 5-HT1 agonist RU 24969 (0.25-5 mg/kg) were studied in rats either after single administrations or after repeated treatment (5 mg/kg per day for 3 days) [33].
  • Using the radioactive microsphere technique in anaesthetized pigs, we studied the systemic and carotid haemodynamic effects of intracarotid infusions (0.3, 1, 3 and 10 micrograms/kg.min) of 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole succinate (RU 24969), a drug with high affinity for 5-HT1A and 5-HT1B recognition sites [3].
  • 2. Exposure to increasing concentrations of 5-methoxy-3(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole succinate (RU 24969) (0.001-0.1 microM) during continuous electrical stimulation produced a concentration-dependent decrease in tritium overflow [34].
  • We have compared the ability of the new putatively specific 5-HT1B receptor agonist CP-93,129 (3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo[3,2-b] pyrid-5-one) and the structurally related mixed 5-HT1A/5-HT1B receptor ligand RU 24969, to influence 5-HT release in brain in vivo, using microdialysis techniques in chloral hydrate-anaesthetised rats [35].
  • GR 127935 blocks the locomotor and antidepressant-like effects of RU 24969 and the action of antidepressants in the mouse tail suspension test [36].


  1. The effects of a 5-HT1 receptor ligand isapirone (TVX Q 7821) on 5-HT synthesis and the behavioural effects of 5-HT agonists in mice and rats. Goodwin, G.M., De Souza, R.J., Green, A.R. Psychopharmacology (Berl.) (1986) [Pubmed]
  2. RU 24969-induced emesis in the cat: 5-HT1 sites other than 5-HT1A, 5-HT1B or 5-HT1C implicated. Lucot, J.B. Eur. J. Pharmacol. (1990) [Pubmed]
  3. The 5-HT1-like receptor mediating reduction of porcine carotid arteriovenous shunting by RU 24969 is not related to either the 5-HT1A or the 5-HT1B subtype. Bom, A.H., Villalón, C.M., Verdouw, P.D., Saxena, P.R. Eur. J. Pharmacol. (1989) [Pubmed]
  4. Stimulation of 5-HT2A receptors in the paraventricular hypothalamus attenuates neuropeptide Y-induced hyperphagia through activation of corticotropin releasing factor. Grignaschi, G., Sironi, F., Samanin, R. Brain Res. (1996) [Pubmed]
  5. The effect of serotonergic agents on haloperidol-induced catalepsy. Hicks, P.B. Life Sci. (1990) [Pubmed]
  6. A behavioural and biochemical study in mice and rats of putative selective agonists and antagonists for 5-HT1 and 5-HT2 receptors. Goodwin, G.M., Green, A.R. Br. J. Pharmacol. (1985) [Pubmed]
  7. The behavioural effects of RU 24969, a suggested 5-HT1 receptor agonist in rodents and the effect on the behaviour of treatment with antidepressants. Green, A.R., Guy, A.P., Gardner, C.R. Neuropharmacology (1984) [Pubmed]
  8. 5-HT1-like receptor agonists enhance wakefulness. Dzoljic, M.R., Ukponmwan, O.E., Saxena, P.R. Neuropharmacology (1992) [Pubmed]
  9. Serotonin1B receptor stimulation enhances cocaine reinforcement. Parsons, L.H., Weiss, F., Koob, G.F. J. Neurosci. (1998) [Pubmed]
  10. Pharmacology of 5-hydroxytryptamine-1A receptors which inhibit cAMP production in hippocampal and cortical neurons in primary culture. Dumuis, A., Sebben, M., Bockaert, J. Mol. Pharmacol. (1988) [Pubmed]
  11. Drug-induced regulation of [125I]iodocyanopindolol-labeled 5-hydroxytryptamine1B receptor binding sites in the central nervous system. Pranzatelli, M.R., Razi, P. Neuropsychopharmacology (1994) [Pubmed]
  12. Serotonin1B receptor activation mimics behavioral effects of presynaptic serotonin release. Rempel, N.L., Callaway, C.W., Geyer, M.A. Neuropsychopharmacology (1993) [Pubmed]
  13. Neurons in the hypothalamic paraventricular nucleus mediate the serotonergic stimulation of prolactin secretion via 5-HT1c/2 receptors. Rittenhouse, P.A., Levy, A.D., Li, Q., Bethea, C.L., Van de Kar, L.D. Endocrinology (1993) [Pubmed]
  14. GR 127935 reduces basal locomotor activity and prevents RU 24969-, but not D-amphetamine-induced hyperlocomotion, in the Wistar-Kyoto hyperactive (WKHA) rat. Chaouloff, F., Courvoisier, H., Moisan, M.P., Mormède, P. Psychopharmacology (Berl.) (1999) [Pubmed]
  15. 5-HT1B agonists induce anorexia at a postsynaptic site. Kennett, G.A., Dourish, C.T., Curzon, G. Eur. J. Pharmacol. (1987) [Pubmed]
  16. The 5-HT1 receptor agonist RU-24969 decreases 5-hydroxytryptamine (5-HT) release and metabolism in the rat frontal cortex in vitro and in vivo. Brazell, M.P., Marsden, C.A., Nisbet, A.P., Routledge, C. Br. J. Pharmacol. (1985) [Pubmed]
  17. Pharmacological analysis of the behavioural and thermoregulatory effects of the putative 5-HT1 receptor agonist, RU 24969, in the rat. Tricklebank, M.D., Middlemiss, D.N., Neill, J. Neuropharmacology (1986) [Pubmed]
  18. A comparison of the effects of the 5-HT1 agonists TFMPP and RU 24969 on feeding following peripheral or medial hypothalamic injection. Fletcher, P.J., Ming, Z.H., Zack, M.H., Coscina, D.V. Brain Res. (1992) [Pubmed]
  19. Quinpirole attenuates the striatal immediate early gene expression, but not the hyperactivity, induced by the serotonin agonist RU-24969. Cook, D.F., Wirtshafter, D. Brain Res. (2000) [Pubmed]
  20. Characterization of a novel serotonin receptor subtype (5-HT1S) in rat CNS: interaction with a GTP binding protein. Zemlan, F.P., Schwab, E.F. J. Neurochem. (1991) [Pubmed]
  21. Characterization of the 5-hydroxytryptamine receptor modulating the release of 5-[3H]hydroxytryptamine in slices of the human neocortex. Galzin, A.M., Poirier, M.F., Lista, A., Chodkiewicz, J.P., Blier, P., Ramdine, R., Loô, H., Roux, F.X., Redondo, A., Langer, S.Z. J. Neurochem. (1992) [Pubmed]
  22. Opposing roles for 5-HT1B and 5-HT3 receptors in the control of 5-HT release in rat hippocampus in vivo. Martin, K.F., Hannon, S., Phillips, I., Heal, D.J. Br. J. Pharmacol. (1992) [Pubmed]
  23. Neurochemical and behavioural studies with RU-24969 in the rat. Carli, M., Invernizzi, R., Cervo, L., Samanin, R. Psychopharmacology (Berl.) (1988) [Pubmed]
  24. beta-Adrenoceptor blocking agents recognize a subpopulation of serotonin receptors in brain. Pazos, A., Engel, G., Palacios, J.M. Brain Res. (1985) [Pubmed]
  25. Actions and some interactions of 5-HT1A ligands in the elevated X-maze and effects of dorsal raphe lesions. Critchley, M.A., Njung'e, K., Handley, S.L. Psychopharmacology (Berl.) (1992) [Pubmed]
  26. Alpha 2-adrenoceptor subtypes and imidazoline-like binding sites in the rat brain. Brown, C.M., MacKinnon, A.C., McGrath, J.C., Spedding, M., Kilpatrick, A.T. Br. J. Pharmacol. (1990) [Pubmed]
  27. Effects in the X-maze anxiety model of agents acting at 5-HT1 and 5-HT2 receptors. Critchley, M.A., Handley, S.L. Psychopharmacology (Berl.) (1987) [Pubmed]
  28. A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system. Dumuis, A., Bouhelal, R., Sebben, M., Cory, R., Bockaert, J. Mol. Pharmacol. (1988) [Pubmed]
  29. The pharmacology of impulsive behaviour in rats IV: the effects of selective serotonergic agents on a paced fixed consecutive number schedule. Evenden, J.L. Psychopharmacology (Berl.) (1998) [Pubmed]
  30. Neuroendocrine evidence for denervation supersensitivity of serotonin receptors: effects of the 5-HT agonist RU 24969 on corticotropin, corticosterone, prolactin and renin secretion. Van de Kar, L.D., Carnes, M., Maslowski, R.J., Bonadonna, A.M., Rittenhouse, P.A., Kunimoto, K., Piechowski, R.A., Bethea, C.L. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  31. Functional behavioral homology between rat 5-HT1B and guinea pig 5-HT1D receptors in the modulation of prepulse inhibition of startle. Sipes, T.E., Geyer, M.A. Psychopharmacology (Berl.) (1996) [Pubmed]
  32. Cardiovascular properties of a 5-HT1-like receptor agonist, 5-methoxy-3(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole (RU 24969) in normotensive anaesthetized rats. Cherqui, C., Dabire, H., Fournier, B., Schmitt, H. Archives internationales de pharmacodynamie et de thérapie. (1988) [Pubmed]
  33. Tolerance to the serotonin 5-HT1 agonist RU 24969 and effects on dopaminergic behaviour. Oberlander, C., Demassey, Y., Verdu, A., Van de Velde, D., Bardelay, C. Eur. J. Pharmacol. (1987) [Pubmed]
  34. Interaction between 5-HT uptake inhibition and activation of 5-HT autoreceptors by exogenous agonists in rat cerebral cortex slices and synaptosomes. Bonanno, G., Raiteri, M. Naunyn Schmiedebergs Arch. Pharmacol. (1987) [Pubmed]
  35. The putative 5-HT1B receptor agonist CP-93,129 suppresses rat hippocampal 5-HT release in vivo: comparison with RU 24969. Hjorth, S., Tao, R. Eur. J. Pharmacol. (1991) [Pubmed]
  36. GR 127935 blocks the locomotor and antidepressant-like effects of RU 24969 and the action of antidepressants in the mouse tail suspension test. O'Neill, M.F., Fernández, A.G., Palacios, J.M. Pharmacol. Biochem. Behav. (1996) [Pubmed]
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