SB224289 Inhibitor – Sb 224289

SB 224289 is a selective antagonist of 5-HT1B receptor with pKi of 8.2. It is a centrally active following oral administration in vivo. 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.

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.
Vidal-Canta degree GC, Jimenez-Hernandez M, Rocha-Gonzalez HI, Villalon CM, Granados-Soto V, Munoz-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.
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.
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.

Small volumes of SB224289, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5756166 is an inhibitor targeting SB224289. Also known as SB 224289.