SB-616234

Last updated

SB-616234
SB-616234.svg
Clinical data
Other namesSB616234; SB-616,234; SB-616234-A; SB-616234A
Drug class Serotonin 5-HT1B receptor antagonist
ATC code
  • None
Identifiers
  • [6-[(3R,5S)-3,5-dimethylpiperazin-1-yl]-5-methoxy-2,3-dihydroindol-1-yl]-[4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]phenyl]methanone
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
Formula C32H35N5O3
Molar mass 537.664 g·mol−1
3D model (JSmol)
  • C[C@@H]1CN(C[C@@H](N1)C)C2=C(C=C3CCN(C3=C2)C(=O)C4=CC=C(C=C4)C5=C(C=C(C=C5)C6=NOC(=N6)C)C)OC
  • InChI=1S/C32H35N5O3/c1-19-14-26(31-34-22(4)40-35-31)10-11-27(19)23-6-8-24(9-7-23)32(38)37-13-12-25-15-30(39-5)29(16-28(25)37)36-17-20(2)33-21(3)18-36/h6-11,14-16,20-21,33H,12-13,17-18H2,1-5H3/t20-,21+
  • Key:QNLSCNDZNSALTM-OYRHEFFESA-N

SB-616234 is a selective serotonin 5-HT1B receptor antagonist. [1] [2] [3] [4] In terms of affinity, it shows 50-fold selectivity for the serotonin 5-HT1B receptor over the serotonin 5-HT1D receptor and greater than 100-fold selectivity for the serotonin 5-HT1B receptor over other serotonin receptors. [3] The drug is a silent antagonist of the serotonin 5-HT1B receptor. [3] It dose-dependently increases serotonin levels in the dentate gyrus of the hippocampus in rodents via blockade of serotonin 5-HT1B autoreceptors. [2] In addition, it augments the increased serotonin levels induced by the selective serotonin reuptake inhibitor (SSRI) paroxetine in this brain area in rodents. [2] The drug produces antidepressant- and anxiolytic-like effects in rodents and anxiolytic-like effects in monkeys. [2] It is orally active. [2] [3] SB-616234 was first described in the scientific literature by 2003. [5] [6] [7]

References

  1. ↑ Wyman PA, Marshall HR, Flynn ST, King RJ, Thompson M, Smith PW, et al. (November 2005). "Identification of a potent and selective 5-HT1B receptor antagonist". Bioorganic & Medicinal Chemistry Letters. 15 (21): 4708–4712. doi:10.1016/j.bmcl.2005.07.085. PMID   16153839.
  2. 1 2 3 4 5 Dawson LA, Hughes ZA, Starr KR, Storey JD, Bettelini L, Bacchi F, et al. (June 2006). "Characterisation of the selective 5-HT1B receptor antagonist SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): in vivo neurochemical and behavioural evidence of anxiolytic/antidepressant activity". Neuropharmacology. 50 (8): 975–983. doi:10.1016/j.neuropharm.2006.01.010. PMID   16581092.
  3. 1 2 3 4 Scott C, Langmead CJ, Clarke KL, Wyman P, Smith PW, Starr KR, et al. (June 2006). "SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2'methyl-4'-(5-methyl-1,2,3-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): a novel, potent and selective 5-HT1B receptor antagonist". Neuropharmacology. 50 (8): 984–990. doi:10.1016/j.neuropharm.2006.01.008. PMID   16546225.
  4. ↑ "Delving into the Latest Updates on SB-616234 with Synapse". Synapse. 25 October 2025. Retrieved 26 January 2026.
  5. ↑ Watson J, Scott C, Langmead C, Wyman P, Smith P, Dawson L, et al. (2003). "P.3.072 SB-616234-A — a novel, potent and selective 5-HT1B receptor antagonist". European Neuropsychopharmacology. 13: S385. doi:10.1016/S0924-977X(03)92192-4 . Retrieved 26 January 2026.
  6. ↑ Hughes Z, Bettelini L, Trail B, Arban R, Dawson L (2003). "P.3.073 The novel and selective 5-HT1B receptor antagonist SB-616234-A increases extracellular 5-HT and displays anxiolytic efficacy in guinea pigs". European Neuropsychopharmacology. 13. Elsevier BV: S385–S386. doi:10.1016/s0924-977x(03)92193-6. ISSN   0924-977X.
  7. ↑ Arban R, Poffe A, Bettelini L, Bacchi F, Gerrard P, Melotto S (2003). "P.3.074 In vivo pharmacological profile of SB-616234-A, a selective 5-HT1B receptor antagonist, in animal models of anxiety and antidepressant-like behaviour". European Neuropsychopharmacology. 13: S386. doi:10.1016/S0924-977X(03)92194-8.
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