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Chemical Compound Review

Isamoltane     1-(propan-2-ylamino)-3-(2- pyrrol-1...

Synonyms: SureCN10697990, AR-1E5090, AC1L2RY1, AC1Q3F4K
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High impact information on Isamoltan

  • Propranolol reduced exercise heart rate by 11% (compared with placebo), 10 mg isamoltane reduced heart rate by 5%, and 4 mg isamoltane reduced heart rate by 1% [1].
  • In conclusion, low-dose isamoltane caused measurable systemic effects on both beta 2- and beta 1-adrenergic receptors, and the dose-dependent blockade on beta 2-receptors of skeletal muscle was more clear than the attenuation of exercise heart rate [1].
  • Pretreating the tissues with the 5-HT1B-selective antagonist isamoltane (200 microM) and the 5-HT2B-selective antagonist rauwolscine (200 microM) inhibited the rapid transient phase by 55 and 45 %, whereas the sustained phase could only be blocked by rauwolscine [2].
  • In the present study, we compared the pharmacology of (+/-)pindolol, WAY-100635 (a 5-HT(1A) antagonist), GR127935 (a 5-HT(1B/1D) antagonist), and isamoltane (a 5-HT(1B) antagonist), when given acutely in combination with fluoxetine, using in vivo microdialysis in the frontal cortex of the freely moving rat [3].
  • These responses were effectively blocked by the 5-HT1B receptor antagonist, isamoltane, the 5-HT1B/5-HT2 receptor antagonist, methiothepin, and the eNOS selective antagonists (0.01-10 microM): L-Nomega -monomethyl-L-arginine (L-NMMA) and L-N omega-iminoethyl-L-ornithine (L-NIO) [4].

Anatomical context of Isamoltan

  • 4. Isamoltane (10(-6) M), the putative 5-HT1B receptor antagonist, blocked the responses to RU24969 (10(-6) M) and 1-(m-trifluoromethylphenyl)piperazine (10(-6) M) in the suprachiasmatic nucleus [5].
  • METHODS: The effects of intracisternal injection of 0.3 mL of arterial blood, artificial cerebrospinal fluid, and 5-HT on rCBF and the levels of 20-HETE and 5-HT in cerebrospinal fluid were measured in rats pretreated with vehicle, a 5-HT1B receptor antagonist (isamoltane hemifumarate), or an inhibitor of the synthesis of 20-HETE (HET0016) [6].

Associations of Isamoltan with other chemical compounds

  • CP 93129 (0.3 microM), the selective 5-HT1B agonist, decreased 5-HT efflux to 37 +/- 4% of control and was antagonised by the 5-HT1B blocker isamoltane (0.5 microM) and by the 5-HT1D/B antagonist GR 127935 (50 nM) [7].
  • SB224289, GR55562, GR127935, isamoltane and metergoline, selective and non-selective 5-HT1B receptor antagonists, in contrast, used at a concentration of 1 microM, antagonized the inhibitory effect of CP93,129 (3 microM and 10 microM) [8].
  • This citalopram (10.0)/WAY-100635 (0.04)-induced effect was fully antagonized by the administration of the 5-HT1B receptor antagonist isamoltane (4.0 mg kg(-1)) [9].
  • This inhibition was prevented by the H3R antagonist thioperamide but not by the 5-HT1B receptor antagonist isamoltane [10].

Gene context of Isamoltan

  • In binding experiments isamoltane was found to be about five times more potent as a ligand for the 5-HT1B receptor than for the 5-HT1A receptor (Ki values 21 and 112 nmol/l, respectively) [11].


  1. Assessment of beta-adrenergic receptor blockade after isamoltane, a 5-HT1-receptor active compound, in healthy volunteers. Bauer, K., Dietersdorfer, F., Kaik, G. Clin. Pharmacol. Ther. (1993) [Pubmed]
  2. Serotonin via 5-HT1B and 5-HT2B receptors stimulates anion secretion in the rat epididymal epithelium. Leung, G.P., Dun, S.L., Dun, N.J., Wong, P.Y. J. Physiol. (Lond.) (1999) [Pubmed]
  3. The role of 5-HT(1A) and 5-HT(1B/1D) receptors on the modulation of acute fluoxetine-induced changes in extracellular 5-HT: the mechanism of action of (+/-)pindolol. Dawson, L.A., Nguyen, H.Q. Neuropharmacology (2000) [Pubmed]
  4. 5-hydroxytryptamine evokes endothelial nitric oxide synthase activation in bovine aortic endothelial cell cultures. McDuffie, J.E., Coaxum, S.D., Maleque, M.A. Proc. Soc. Exp. Biol. Med. (1999) [Pubmed]
  5. Pharmacological characteristics of 5-hydroxytryptamine autoreceptors in rat brain slices incorporating the dorsal raphe or the suprachiasmatic nucleus. O'Connor, J.J., Kruk, Z.L. Br. J. Pharmacol. (1992) [Pubmed]
  6. Contribution of 5-hydroxytryptamine1B receptors and 20-hydroxyeiscosatetraenoic acid to fall in cerebral blood flow after subarachnoid hemorrhage. Cambj-Sapunar, L., Yu, M., Harder, D.R., Roman, R.J. Stroke (2003) [Pubmed]
  7. Serotonin efflux in the rat ventral lateral geniculate nucleus assessed by fast cyclic voltammetry is modulated by 5-HT1B and 5-HT1D autoreceptors. Davidson, C., Stamford, J.A. Neuropharmacology (1996) [Pubmed]
  8. 5-HT1B receptors modulate release of [3H]dopamine from rat striatal synaptosomes. Sarhan, H., Cloëz-Tayarani, I., Massot, O., Fillion, M.P., Fillion, G. Naunyn Schmiedebergs Arch. Pharmacol. (1999) [Pubmed]
  9. Synergistic actions of the 5-HT1A receptor antagonist WAY-100635 and citalopram on male rat ejaculatory behavior. Ahlenius, S., Larsson, K. Eur. J. Pharmacol. (1999) [Pubmed]
  10. Histamine H3 receptors inhibit serotonin release in substantia nigra pars reticulata. Threlfell, S., Cragg, S.J., Kalló, I., Turi, G.F., Coen, C.W., Greenfield, S.A. J. Neurosci. (2004) [Pubmed]
  11. Biochemical and behavioural effects of isamoltane, a beta-adrenoceptor antagonist with affinity for the 5-HT1B receptor of rat brain. Rényi, L., Larsson, L.G., Berg, S., Svensson, B.E., Thorell, G., Ross, S.B. Naunyn Schmiedebergs Arch. Pharmacol. (1991) [Pubmed]
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