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Chemical Compound Review

Tocris-1032     9-(1,2,3,6-tetrahydropyridin- 4-yl)-2,7...

Synonyms: CHEMBL304008, SureCN781544, SureCN9696192, CHEBI:202053, LS-184387, ...
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Disease relevance of CP 93129

  • Pertussis toxin pretreatment blocked the CP 93,129-induced inhibition of FSCA and elevation of [Ca2+]i in OK cells, indicating the involvement of Gi/o proteins in transducing these second messenger responses [1].

Psychiatry related information on CP 93129


High impact information on CP 93129


Chemical compound and disease context of CP 93129


Biological context of CP 93129

  • The selective 5-HT1B receptor agonist 1,4-dihydro-3-(1,2,3,6-tetrahydro-4-pyridinyl)-5H-pyrrolo[3,2-b]pyridin-5-one dihydrochloride (CP 93129, 300 micro m) reduced dialysate 5-HT to the same extent (30-40% of baseline) in the two genotypes, which suggests a lack of compensatory changes in 5-HT1B receptors in the DR of such mutant mice [8].
  • CP-93,129 also decreased food intake when injected into the hypothalamic paraventricular nucleus, but this action was 50-fold less potent than administration into the PBN [9].
  • In addition, by blocking the 5-HT1B sites with 100 nM CP 93129, the remaining population of [125I]GTI binding sites could be studied and was found to have high affinity for PAPP, rauwolscine and 8-OH-DPAT [10].
  • Micromolar concentrations of the 5-HT1B receptor agonist 3-(1,2,5,6-tetrahydro)-4-pyridil-5-pyrrolo[3,2-b]pyril-5-one (CP 93,129) and of the 5-HT2 receptor agonist 1-(2,5-dimethoxy-4-iodophenyl_-2-aminopropane (DOI) induced cell growth with a potency that accorded with the affinity of these compounds for the human 5-HT1D receptor site [11].
  • CP-93,129 also increased blood pressure and reduced heart rate [12].

Anatomical context of CP 93129


Associations of CP 93129 with other chemical compounds


Gene context of CP 93129

  • Intra-tegmental infusion of CP 93129 (20, 40, and 80 microM), a 5-HT1B receptor agonist, increased extracellular DA concentrations in a concentration-dependent manner not only in the NACC but also in the VTA, indicating increased mesolimbic DA neuron activity [21].
  • The selective 5-HT1B antagonist SB-224289 inhibited GTI- and CP 93129-stimulated [35S]GTPgammaS binding in basal ganglia and substantia nigra, while coincubation with BRL 15572 (selective 5-HT1D antagonist) did not result in any significant change [13].
  • Intrathecal administration of a 5-HT1A receptor agonist, 8-hydroxy-2-(di-n-propylamino)-tetraline (8-OH-DPAT; 1, 10, and 30 microg), or a 5-HT1B receptor agonist, 1, 4-dihydro-3-(1, 2, 3, 6-tetrahydro-4-pyridinyl)-5H-pyrrol (3, 2-b) pyridin-5-one (CP 93129; 1 and 10 microg), produced no significant change in the number of flinches [22].
  • ICV injections of CP-93,129 (100 micrograms/kg) increased the plasma concentrations of ACTH, prolactin, and renin [12].

Analytical, diagnostic and therapeutic context of CP 93129


  1. Native 5-HT1B receptors expressed in OK cells display dual coupling to elevation of intracellular calcium concentrations and inhibition of adenylate cyclase. Zgombick, J.M., Branchek, T.A. Naunyn Schmiedebergs Arch. Pharmacol. (1998) [Pubmed]
  2. Subthalamic 5-HT(1A) and 5-HT(1B) receptor modulation of RU 24969-induced behavioral profile in rats. Martinez-Price, D.L., Geyer, M.A. Pharmacol. Biochem. Behav. (2002) [Pubmed]
  3. 5-Carboxamido-tryptamine, CP-122,288 and dihydroergotamine but not sumatriptan, CP-93,129, and serotonin-5-O-carboxymethyl-glycyl -tyrosinamide block dural plasma protein extravasation in knockout mice that lack 5-hydroxytryptamine1B receptors. Yu, X.J., Waeber, C., Castanon, N., Scearce, K., Hen, R., Macor, J.E., Chauveau, J., Moskowitz, M.A., Chaveau, J. Mol. Pharmacol. (1996) [Pubmed]
  4. The modulation by 5-HT of glutamatergic inputs from the raphe pallidus to rat hypoglossal motoneurones, in vitro. Bouryi, V.A., Lewis, D.I. J. Physiol. (Lond.) (2003) [Pubmed]
  5. The role of 5-HT1B receptors in the regulation of serotonin cell firing and release in the rat brain. Adell, A., Celada, P., Artigas, F. J. Neurochem. (2001) [Pubmed]
  6. Regulation of serotonin release in the frontal cortex and ventral hippocampus of homozygous mice lacking 5-HT1B receptors: in vivo microdialysis studies. Trillat, A.C., Malagié, I., Scearce, K., Pons, D., Anmella, M.C., Jacquot, C., Hen, R., Gardier, A.M. J. Neurochem. (1997) [Pubmed]
  7. Effects of 5-HT1B receptor ligands microinjected into the accumbal shell or core on the cocaine-induced locomotor hyperactivity in rats. Przegaliński, E., Filip, M., Papla, I., Czepiel, K. J. Physiol. Pharmacol. (2002) [Pubmed]
  8. In vivo efflux of serotonin in the dorsal raphe nucleus of 5-HT1A receptor knockout mice. Bortolozzi, A., Amargós-Bosch, M., Toth, M., Artigas, F., Adell, A. J. Neurochem. (2004) [Pubmed]
  9. Infusion of the serotonin1B (5-HT1B) agonist CP-93,129 into the parabrachial nucleus potently and selectively reduces food intake in rats. Lee, M.D., Aloyo, V.J., Fluharty, S.J., Simansky, K.J. Psychopharmacology (Berl.) (1998) [Pubmed]
  10. Autoradiographic characterisation and localisation of 5-HT1D compared to 5-HT1B binding sites in rat brain. Bruinvels, A.T., Palacios, J.M., Hoyer, D. Naunyn Schmiedebergs Arch. Pharmacol. (1993) [Pubmed]
  11. Promotion of cell growth by stimulation of cloned human 5-HT1D receptor sites in transfected C6-glial cells is highly sensitive to intrinsic activity at 5-HT1D receptors. Pauwels, P.J., Wurch, T., Palmier, C., Colpaert, F.C. Naunyn Schmiedebergs Arch. Pharmacol. (1996) [Pubmed]
  12. ICV injection of the serotonin 5-HT1B agonist CP-93,129 increases the secretion of ACTH, prolactin, and renin and increases blood pressure by nonserotonergic mechanisms. Van de Kar, L.D., Alvarez Sanz, M.C., Yracheta, J.M., Kunimoto, K., Li, Q., Levy, A.D., Rittenhouse, P.A. Pharmacol. Biochem. Behav. (1994) [Pubmed]
  13. Autoradiographic characterisation of [35S]GTPgammaS binding stimulation mediated by 5-HT1B receptor in postmortem human brain. Mostany, R., Pazos, A., Castro, M.E. Neuropharmacology (2005) [Pubmed]
  14. The 5HT(1B) receptor agonist, CP-93129, inhibits [(3)H]-GABA release from rat globus pallidus slices and reverses akinesia following intrapallidal injection in the reserpine-treated rat. Chadha, A., Sur, C., Atack, J., Duty, S. Br. J. Pharmacol. (2000) [Pubmed]
  15. CP-93,129, a potent and selective 5-HT1B receptor agonist blocks neurogenic plasma extravasation within rat but not guinea-pig dura mater. Matsubara, T., Moskowitz, M.A., Byun, B. Br. J. Pharmacol. (1991) [Pubmed]
  16. Selective 5-HT1B receptor agonist reduces serotonin synthesis following acute, and not chronic, drug administration: results of an autoradiographic study. Hasegawa, S., Watanabe, A., Nishi, K., Nguyen, K.Q., Diksic, M. Neurochem. Int. (2005) [Pubmed]
  17. Presynaptic inhibition by 5-HT1B receptors of glutamatergic synaptic inputs onto serotonergic caudal raphe neurones in rat. Li, Y.W., Bayliss, D.A. J. Physiol. (Lond.) (1998) [Pubmed]
  18. Release of immunoreactive substance P in the brain stem upon stimulation of the cranial dura mater with low pH - inhibition by the serotonin (5-HT1) receptor agonist CP 93,129. Messlinger, K., Ebersberger, A., Schaible, H.G. Br. J. Pharmacol. (1998) [Pubmed]
  19. Serotonin-mediated increase in prefrontal cortex dopamine release: pharmacological characterization. Iyer, R.N., Bradberry, C.W. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  20. Effect of a 5-HT1 receptor agonist, CP-122,288, on oedema formation induced by stimulation of the rat saphenous nerve. Kajekar, R., Gupta, P., Shepperson, N.B., Brain, S.D. Br. J. Pharmacol. (1995) [Pubmed]
  21. Involvement of 5-HT1B receptors within the ventral tegmental area in regulation of mesolimbic dopaminergic neuronal activity via GABA mechanisms: a study with dual-probe microdialysis. Yan, Q.S., Zheng, S.Z., Yan, S.E. Brain Res. (2004) [Pubmed]
  22. Effects of 5-HT2 and 5-HT3 receptors on the modulation of nociceptive transmission in rat spinal cord according to the formalin test. Sasaki, M., Ishizaki, K., Obata, H., Goto, F. Eur. J. Pharmacol. (2001) [Pubmed]
  23. Spatial memory deficits following stimulation of hippocampal 5-HT1B receptors in the rat. Buhot, M.C., Patra, S.K., Naïli, S. Eur. J. Pharmacol. (1995) [Pubmed]
  24. An antagonistic 5-HT receptor system in the auricles of the systemic heart complex of Sepia officinalis L. (Cephalopoda) shows 5-HT1 and 5-HT4 subtype properties. Lehr, T., Schipp, R. Comp. Biochem. Physiol. C Toxicol. Pharmacol. (2004) [Pubmed]
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