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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. ^ a b c d e 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. ^ a b c d 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.