CAS No. : 180083-23-2

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:M035366
Molecular Formula:C32H32N4O3
Molecular Weight:520.633
Target:5-HT1B receptor antagonist
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Appearance:Solid powder
Purity: > 98%
Cat No:M035366
Cas No:180083-23-2
IUPAC Name:[4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]phenyl]-(1/'-methylspiro[6,7-dihydro-2H-furo[2,3-f]indole-3,4/'-piperidine]-5-yl)methanone
SB 224289 is a selective 5-HT1B receptor antagonist (pKi = 8.2). SB 224289 displays > 60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand binding and functional assays. SB 224289 is a centrally active following oral administration in vivo.

1: Cassilly CD, Maddox MM, Cherian PT, Bowling JJ, Hamann MT, Lee RE, Reynolds TB. SB-224289 Antagonizes the Antifungal Mechanism of the Marine Depsipeptide Papuamide A. PLoS One. 2016 May 16;11(5):e0154932. doi: 10.1371/journal.pone.0154932. PubMed PMID: 27183222; PubMed Central PMCID: PMC4868317.
2: Vidal-Cantú GC, Jiménez-Hernández M, Rocha-González HI, Villalón CM, Granados-Soto V, Muñoz-Islas E. Role of 5-HT5A and 5-HT1B/1D receptors in the antinociception produced by ergotamine and valerenic acid in the rat formalin test. Eur J Pharmacol. 2016 Jun 15;781:109-16. doi: 10.1016/j.ejphar.2016.04.009. PubMed PMID: 27068146.
3: Kim JM, Jeong SW, Yang J, Lee SH, Kim WM, Jeong S, Bae HB, Yoon MH, Choi JI. Spinal 5-HT1A, not the 5-HT1B or 5-HT3 receptors, mediates descending serotonergic inhibition for late-phase mechanical allodynia of carrageenan-induced peripheral inflammation. Neurosci Lett. 2015 Jul 23;600:91-7. doi: 10.1016/j.neulet.2015.05.058. PubMed PMID: 26037417.
4: Maximino C, Lima MG, Batista Ede J, Oliveira KR, Herculano AM. Interaction between 5-HT1B receptors and nitric oxide in zebrafish responses to novelty. Neurosci Lett. 2015 Feb 19;588:54-6. doi: 10.1016/j.neulet.2014.12.049. PubMed PMID: 25545556.
5: Hall FS, Sora I, Hen R, Uhl GR. Serotonin/dopamine interactions in a hyperactive mouse: reduced serotonin receptor 1B activity reverses effects of dopamine transporter knockout. PLoS One. 2014 Dec 16;9(12):e115009. doi: 10.1371/journal.pone.0115009. PubMed PMID: 25514162; PubMed Central PMCID: PMC4267809.
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7: Chan KY, Labruijere S, Ramírez Rosas MB, de Vries R, Garrelds IM, Danser AH, Villalón CM, van den Bogaerdt A, Dirven C, MaassenVanDenBrink A. Cranioselectivity of sumatriptan revisited: pronounced contractions to sumatriptan in small human isolated coronary artery. CNS Drugs. 2014 Mar;28(3):273-8. doi: 10.1007/s40263-013-0136-0. PubMed PMID: 24430784.
8: Pentkowski NS, Harder BG, Brunwasser SJ, Bastle RM, Peartree NA, Yanamandra K, Adams MD, Der-Ghazarian T, Neisewander JL. Pharmacological evidence for an abstinence-induced switch in 5-HT1B receptor modulation of cocaine self-administration and cocaine-seeking behavior. ACS Chem Neurosci. 2014 Mar 19;5(3):168-76. doi: 10.1021/cn400155t. PubMed PMID: 24369697; PubMed Central PMCID: PMC3986226.
9: Liao CC, Lee LJ. Presynaptic 5-HT1B receptor-mediated synaptic suppression to the subplate neurons in the somatosensory cortex of neonatal rats. Neuropharmacology. 2014 Feb;77:81-9. doi: 10.1016/j.neuropharm.2013.08.040. PubMed PMID: 24055501.
10: Quiñonez-Bastidas GN, Cervantes-Durán C, Rocha-González HI, Murbartián J, Granados-Soto V. Analysis of the mechanisms underlying the antinociceptive effect of epicatechin in diabetic rats. Life Sci. 2013 Oct 17;93(17):637-45. doi: 10.1016/j.lfs.2013.08.022. PubMed PMID: 24012613.
11: Cervantes-Durán C, Rocha-González HI, Granados-Soto V. Peripheral and spinal 5-HT receptors participate in the pronociceptive and antinociceptive effects of fluoxetine in rats. Neuroscience. 2013 Nov 12;252:396-409. doi: 10.1016/j.neuroscience.2013.08.022. PubMed PMID: 23994595.
12: Godínez-Chaparro B, López-Santillán FJ, Argüelles CF, Villalón CM, Granados-Soto V. Role of 5-HT₁B/₁D receptors in the reduction of formalin-induced nociception and secondary allodynia/hyperalgesia produced by antimigraine drugs in rats. Life Sci. 2013 Jun 13;92(22):1046-54. doi: 10.1016/j.lfs.2013.03.023. PubMed PMID: 23583574.
13: Maximino C, Puty B, Benzecry R, Araújo J, Lima MG, de Jesus Oliveira Batista E, Renata de Matos Oliveira K, Crespo-Lopez ME, Herculano AM. Role of serotonin in zebrafish (Danio rerio) anxiety: relationship with serotonin levels and effect of buspirone, WAY 100635, SB 224289, fluoxetine and para-chlorophenylalanine (pCPA) in two behavioral models. Neuropharmacology. 2013 Aug;71:83-97. doi: 10.1016/j.neuropharm.2013.03.006. PubMed PMID: 23541719.
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16: Silva SA, Ribeiro CA. Tachyphylaxis to the sumatriptan-induced contractile effect in the human uterine artery but not in human cerebral blood vessels: pharmacological demonstration of the 5-HT(1B) receptor functionality loss. Pharmacology. 2012;89(1-2):29-36. doi: 10.1159/000334930. PubMed PMID: 22302025.
17: Solati J, Salari AA, Bakhtiari A. 5HT(1A) and 5HT(1B) receptors of medial prefrontal cortex modulate anxiogenic-like behaviors in rats. Neurosci Lett. 2011 Oct 31;504(3):325-9. doi: 10.1016/j.neulet.2011.09.058. PubMed PMID: 21982809.
18: Janhunen SK, van der Zwaal EM, la Fleur SE, Adan RA. Inverse agonism at α2A adrenoceptors augments the hypophagic effect of sibutramine in rats. Obesity (Silver Spring). 2011 Oct;19(10):1979-86. doi: 10.1038/oby.2011.51. PubMed PMID: 21475142.
19: Nakamura E, Tanaka N, Kuwabara M, Yamashita A, Matsuo Y, Kanai T, Onitsuka T, Asada Y, Hisa H, Yamamoto R. Relative contributions of 5-hydroxytryptamine (5-HT) receptor subtypes in 5-HT-induced vasoconstriction of the distended human saphenous vein as a coronary artery bypass graft. Biol Pharm Bull. 2011;34(1):82-6. PubMed PMID: 21212522.
20: Aira Z, Buesa I, Salgueiro M, Bilbao J, Aguilera L, Zimmermann M, Azkue JJ. Subtype-specific changes in 5-HT receptor-mediated modulation of C fibre-evoked spinal field potentials are triggered by peripheral nerve injury. Neuroscience. 2010 Jul 14;168(3):831-41. doi: 10.1016/j.neuroscience.2010.04.032. PubMed PMID: 20412834.

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