Elzasonan

Chemical compound
  • none
Legal statusLegal status
  • In general: uncontrolled
Identifiers
  • 4-(3,4-dichlorophenyl)-2-[2-(4-methylpiperazin-1-yl)-benzylidene]-thiomorpholin-3-one
CAS Number
  • 361343-19-3 checkY
  • HCl: 220322-05-4 checkY
PubChem CID
  • 19544192
  • HCl: 6914152
ChemSpider
  • 5290108
UNII
  • 933PJL964R
  • HCl: X38F62RR8L checkY
Chemical and physical dataFormulaC22H23Cl2N3OSMolar mass448.41 g·mol−13D model (JSmol)
  • Interactive image
  • Clc4c(Cl)cc(N1C(=O)C(\SCC1)=C\c3ccccc3N2CCN(C)CC2)cc4
InChI
  • InChI=1S/C22H23Cl2N3OS/c1-25-8-10-26(11-9-25)20-5-3-2-4-16(20)14-21-22(28)27(12-13-29-21)17-6-7-18(23)19(24)15-17/h2-7,14-15H,8-13H2,1H3/b21-14-
  • Key:LHYMPSWMHXUWSK-STZFKDTASA-N
  (verify)

Elzasonan (CP-448,187) is a selective 5-HT1B and 5-HT1D receptor antagonist that was under development by Pfizer for the treatment of depression but was discontinued, possibly due to poor efficacy.[1][2][3][4][5] By preferentially blocking 5-HT1B and 5-HT1D autoreceptors, elzasonan is thought to enhance serotonergic innervations originating from the raphe nucleus, thereby improving signaling to limbic regions like the hippocampus and prefrontal cortex and ultimately resulting in antidepressant effects.[3]

See also

References

  1. ^ Vela JM, Buschmann H, Holenz J, Párraga A, Torrens A (2007). Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application. Weinheim: Wiley-VCH. ISBN 978-3-527-31058-6.
  2. ^ Stahl SM (2008). Stahl's essential psychopharmacology: neuroscientific basis and practical applications. Cambridge, UK: Cambridge University Press. ISBN 978-0-521-85702-4.
  3. ^ a b Dawson LA, Bromidge SM (August 2008). "5-HT1 receptor augmentation strategies as enhanced efficacy: therapeutics for psychiatric disorders". Current Topics in Medicinal Chemistry. 8 (12): 1008–1023. doi:10.2174/156802608785161439. PMID 18691129.
  4. ^ Norman P (2002). "Pfizer, Inc.: analysis of patenting 1998 – 2001". Expert Opinion on Therapeutic Patents. 12 (5): 725–732. doi:10.1517/13543776.12.5.725. S2CID 84645020.
  5. ^ Kirchhoff VD, Nguyen HT, Soczynska JK, Woldeyohannes H, McIntyre RS (October 2009). "Discontinued psychiatric drugs in 2008". Expert Opinion on Investigational Drugs. 18 (10): 1431–1443. doi:10.1517/13543780903184591. PMID 19715445. S2CID 34201544.
  • v
  • t
  • e
SSRIsTooltip Selective serotonin reuptake inhibitors
SNRIsTooltip Serotonin–norepinephrine reuptake inhibitors
NRIsTooltip Norepinephrine reuptake inhibitors
NDRIsTooltip Norepinephrine–dopamine reuptake inhibitors
NaSSAsTooltip Noradrenergic and specific serotonergic antidepressants
SARIsTooltip Serotonin antagonist and reuptake inhibitors
SMSTooltip Serotonin modulator and stimulators
Others
TCAsTooltip Tricyclic antidepressants
TeCAsTooltip Tetracyclic antidepressants
Others
Non-selective
MAOATooltip Monoamine oxidase A-selective
MAOBTooltip Monoamine oxidase B-selective
Miscellaneous
  • v
  • t
  • e
5-HT1ARTooltip 5-HT1A receptor agonists
GABAARTooltip GABAA receptor PAMsTooltip positive allosteric modulators
Hypnotics
Gabapentinoids
(α2δ VDCC blockers)
Antidepressants
Antipsychotics
Sympatholytics
(Antiadrenergics)
Others
  • v
  • t
  • e
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
  • See also: Receptor/signaling modulators
  • Adrenergics
  • Dopaminergics
  • Melatonergics
  • Monoamine reuptake inhibitors and releasing agents
  • Monoamine metabolism modulators
  • Monoamine neurotoxins