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Adatanserin

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Adatanserin

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Adatanserin
Systematic (IUPAC) name
N-[2-(4-pyrimidin-2-ylpiperazin-1-yl)ethyl]adamantane-1-carboxamide
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number 127266-56-2
ATC code None
PubChem CID 130918
ChemSpider 115774 YesY
UNII W5U6WQM26H YesY
Chemical data
Formula C21H31N5O 
Mol. mass 369.50 g/mol
SMILES eMolecules & PubChem
 YesY (what is this?)  (verify)

Adatanserin (WY-50,324, SEB-324) is a mixed 5-HT1A receptor partial agonist and 5-HT2A and 5-HT2C receptor antagonist.[1][2][3] It was under development by Wyeth as an antidepressant but was ultimately shelved.[3][4]

Adantaserin has been shown to be neuroprotective against ischemia-induced glutamatergic excitotoxicity, an effect which appears to be mediated by blockade of the 5-HT2A receptor.[5]

See also

References

  1. ^ Singh A, Lucki I (April 1993). "Antidepressant-like activity of compounds with varying efficacy at 5-HT1A receptors". Neuropharmacology 32 (4): 331–40. doi:10.1016/0028-3908(93)90153-T. PMID 8497336. 
  2. ^ Kleven MS, Koek W (February 1996). "Pharmacological characterization of in vivo properties of putative mixed 5-HT1A agonist/5-HT2A/2C antagonist anxiolytics. I. Antipunishment effects in the pigeon". The Journal of Pharmacology and Experimental Therapeutics 276 (2): 388–97. PMID 8632301. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8632301. 
  3. ^ a b Abou-Gharbia MA, Childers WE, Fletcher H, et al. (December 1999). "Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents". Journal of Medicinal Chemistry 42 (25): 5077–94. doi:10.1021/jm9806704. PMID 10602693. 
  4. ^ Stahl, S. M. (2000). Essential psychopharmacology: neuroscientific basis and practical application. Cambridge, UK: Cambridge University Press. ISBN 0-521-64615-4. http://books.google.com/books?id=ICztBCFFRqEC&lpg=PA262&dq=adatanserin&as_brr=3&pg=PA262#v=onepage&q=adatanserin&f=false. 
  5. ^ Dawson LA, Galandak J, Djali S (March 2002). "Attenuation of ischemic efflux of endogenous amino acids by the novel 5-HT(1A)/5-HT(2) receptor ligand adatanserin". Neurochemistry International 40 (3): 203–9. doi:10.1016/S0197-0186(01)00082-1. PMID 11741003. http://linkinghub.elsevier.com/retrieve/pii/S0197018601000821. 
GABAA PAMs
Abecarnil • Adipiplon • Alpidem • CGS-8216 • CGS-9896 • CGS-13767 • CGS-20625 • Divaplon • ELB-139 • Fasiplon • GBLD-345 • Gedocarnil • L-838,417 • NS-2664 • NS-2710 • Ocinaplon • Pagoclone • Panadiplon • Pipequaline • RWJ-51204 • SB-205,384 • SL-651,498 • Taniplon • TP-003 • TP-13 • TPA-023 • Y-23684 • ZK-93423
Others
α2δ VDCC Blockers
5-HT1A Agonists
Azapirones: Buspirone • Gepirone • Tandospirone; Others: Flesinoxan • Oxaflozane
H1 Antagonists
Diphenylmethanes: Captodiame • Hydroxyzine; Others: Brompheniramine • Chlorpheniramine • Pheniramine
CRH1 Antagonists
NK2 Antagonists
MCH1 antagonists
mGluR2/3 Agonists
mGluR5 NAMs
TSPO agonists
σ1 agonists
Others

M: PSO/PSI

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc(eval/thrp), drug(N5A/5B/5C/6A/6B/6D)

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