Chemistry:SB-616234

From HandWiki

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. ↑ "Identification of a potent and selective 5-HT1B receptor antagonist". Bioorganic & Medicinal Chemistry Letters 15 (21): 4708–4712. November 2005. doi:10.1016/j.bmcl.2005.07.085. PMID 16153839. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 "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. June 2006. doi:10.1016/j.neuropharm.2006.01.010. PMID 16581092. 
  3. ↑ 3.0 3.1 3.2 3.3 "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. June 2006. doi:10.1016/j.neuropharm.2006.01.008. PMID 16546225. 
  4. ↑ "Delving into the Latest Updates on SB-616234 with Synapse". 25 October 2025. https://synapse.patsnap.com/drug/55180489334c435b90c431d662cf5fe9. 
  5. ↑ "P.3.072 SB-616234-A — a novel, potent and selective 5-HT1B receptor antagonist". European Neuropsychopharmacology 13: S385. 2003. doi:10.1016/S0924-977X(03)92192-4. https://linkinghub.elsevier.com/retrieve/pii/S0924977X03921924. Retrieved 26 January 2026. 
  6. ↑ "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 (Elsevier BV) 13: S385–S386. 2003. doi:10.1016/s0924-977x(03)92193-6. ISSN 0924-977X. 
  7. ↑ "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. 2003. doi:10.1016/S0924-977X(03)92194-8. 



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