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SB-699551

SB-699551 is a drug which was the first compound developed to act as a selective antagonist for the serotonin receptor 5-HT5A, with selectivity of around 100x over other serotonin receptor subtypes. Multiple therapeutic roles have been suggested for 5-HT5A ligands due to the presence of this receptor in several areas of the brain, but research is still at an early stage, In animal studies, SB-699551 was found to block cue-mediated responding to LSD, again suggesting an antipsychotic type of activity. It also reduces the viability of certain types of cancer cells in vitro, suggesting the 5-HT5A receptor as a possible target for novel chemotherapy drugs.

SB-699551
Identifiers
IUPAC name
  • 3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-([(2-phenylethyl)amino]methyl)-4-biphenylyl)methyl]propanamide
CAS Number
PubChemCID
ChemSpider
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC34H45N3O
Molar mass511.754 g·mol−1
3D model (JSmol)
  • C2CCCC2CCC(=O)N(CCN(C)C)Cc(cc3)ccc3-c(cc1)ccc1CNCCc4ccccc4
  • InChI=1S/C34H45N3O/c1-36(2)24-25-37(34(38)21-16-28-10-6-7-11-28)27-31-14-19-33(20-15-31)32-17-12-30(13-18-32)26-35-23-22-29-8-4-3-5-9-29/h3-5,8-9,12-15,17-20,28,35H,6-7,10-11,16,21-27H2,1-2H3
  • Key:SEQAMPXQRKYYQF-UHFFFAOYSA-N
(verify)
  1. Thomas DR, Soffin EM, Roberts C, Kew JN, de la Flor RM, Dawson LA, et al. (September 2006). "SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain". Neuropharmacology. 51 (3): 566–77. doi:10.1016/j.neuropharm.2006.04.019. PMID 16846620.
  2. Nikiforuk A, Hołuj M, Kos T, Popik P (June 2016). "The effects of a 5-HT5A receptor antagonist in a ketamine-based rat model of cognitive dysfunction and the negative symptoms of schizophrenia". Neuropharmacology. 105: 351–360. doi:10.1016/j.neuropharm.2016.01.035. PMID 26826431.
  3. Popik P, Krawczyk M, Kuziak A, Bugno R, Hogendorf A, Staroń J, Nikiforuk A (August 2019). "Serotonin type 5A receptor antagonists inhibit D-lysergic acid diethylamide discriminatory cue in rats". Journal of Psychopharmacology: 269881119867603. doi:10.1177/0269881119867603. PMID 31452444.
  4. Itsumi M, Shiota M, Sekino Y, et al. High-throughput screen identifies 5-HT receptor as a modulator of AR and a therapeutic target for prostate cancer. Prostate. 2020;80(11):885-894. doi:10.1002/pros.24022
  5. Gwynne WD, Shakeel MS, Girgis-Gabardo A, et al. Antagonists of the serotonin receptor 5A target human breast tumor initiating cells. BMC Cancer. 2020;20(1):724. doi:10.1186/s12885-020-07193-6

SB-699551
SB 699551 Language Watch Edit 160 160 Redirected from SB 699 551 SB 699551 is a drug which was the first compound developed to act as a selective antagonist for the serotonin receptor 5 HT5A with selectivity of around 100x over other serotonin receptor subtypes 1 Multiple therapeutic roles have been suggested for 5 HT5A ligands due to the presence of this receptor in several areas of the brain but research is still at an early stage 2 In animal studies SB 699551 was found to block cue mediated responding to LSD again suggesting an antipsychotic type of activity 3 It also reduces the viability of certain types of cancer cells in vitro suggesting the 5 HT5A receptor as a possible target for novel chemotherapy drugs 4 5 SB 699551IdentifiersIUPAC name 3 cyclopentyl N 2 dimethylamino ethyl N 4 2 phenylethyl amino methyl 4 biphenylyl methyl propanamideCAS Number791789 61 2 YPubChem CID11168182ChemSpider9343277CompTox Dashboard EPA DTXSID90457468Chemical and physical dataFormulaC 34H 45N 3OMolar mass511 754 g mol 13D model JSmol Interactive imageSMILES C2CCCC2CCC O N CCN C C Cc cc3 ccc3 c cc1 ccc1CNCCc4ccccc4InChI InChI 1S C34H45N3O c1 36 2 24 25 37 34 38 21 16 28 10 6 7 11 28 27 31 14 19 33 20 15 31 32 17 12 30 13 18 32 26 35 23 22 29 8 4 3 5 9 29 h3 5 8 9 12 15 17 20 28 35H 6 7 10 11 16 21 27H2 1 2H3Key SEQAMPXQRKYYQF UHFFFAOYSA N verify References Edit Thomas DR Soffin EM Roberts C Kew JN de la Flor RM Dawson LA et al September 2006 SB 699551 A 3 cyclopentyl N 2 dimethylamino ethyl N 4 2 phenylethyl amino methyl 4 biphenylyl methyl propanamide dihydrochloride a novel 5 ht5A receptor selective antagonist enhances 5 HT neuronal function Evidence for an autoreceptor role for the 5 ht5A receptor in guinea pig brain Neuropharmacology 51 3 566 77 doi 10 1016 j neuropharm 2006 04 019 PMID 16846620 Nikiforuk A Holuj M Kos T Popik P June 2016 The effects of a 5 HT5A receptor antagonist in a ketamine based rat model of cognitive dysfunction and the negative symptoms of schizophrenia Neuropharmacology 105 351 360 doi 10 1016 j neuropharm 2016 01 035 PMID 26826431 Popik P Krawczyk M Kuziak A Bugno R Hogendorf A Staron J Nikiforuk A August 2019 Serotonin type 5A receptor antagonists inhibit D lysergic acid diethylamide discriminatory cue in rats Journal of Psychopharmacology 269881119867603 doi 10 1177 0269881119867603 PMID 31452444 Itsumi M Shiota M Sekino Y et al High throughput screen identifies 5 HT receptor as a modulator of AR and a therapeutic target for prostate cancer Prostate 2020 80 11 885 894 doi 10 1002 pros 24022 Gwynne WD Shakeel MS Girgis Gabardo A et al Antagonists of the serotonin receptor 5A target human breast tumor initiating cells BMC Cancer 2020 20 1 724 doi 10 1186 s12885 020 07193 6 This drug article relating to the nervous system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title SB 699551 amp oldid 977677502, wikipedia, wiki, book,

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