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SRX251

From Wikipedia, the free encyclopedia

Pharmaceutical compound
SRX251
Clinical data
Other namesSRX-251; API-251; API251
Routes of
administration
Oral[1][2]
Drug classVasopressinV1A receptorantagonist
Identifiers
  • (2R)-N-methyl-4-oxo-2-[(3S,4R)-2-oxo-3-[(4S)-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]-4-[(E)-2-phenylethenyl]azetidin-1-yl]-4-(4-piperidin-1-ylpiperidin-1-yl)-N-[[3-(trifluoromethyl)phenyl]methyl]butanamide
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC43H48F3N5O5
Molar mass771.882 g·mol−1
3D model (JSmol)
  • CN(CC1=CC(=CC=C1)C(F)(F)F)C(=O)[C@@H](CC(=O)N2CCC(CC2)N3CCCCC3)N4[C@@H]([C@@H](C4=O)N5[C@H](COC5=O)C6=CC=CC=C6)/C=C/C7=CC=CC=C7
  • InChI=1S/C43H48F3N5O5/c1-47(28-31-14-11-17-33(26-31)43(44,45)46)40(53)36(27-38(52)49-24-20-34(21-25-49)48-22-9-4-10-23-48)50-35(19-18-30-12-5-2-6-13-30)39(41(50)54)51-37(29-56-42(51)55)32-15-7-3-8-16-32/h2-3,5-8,11-19,26,34-37,39H,4,9-10,20-25,27-29H2,1H3/b19-18+/t35-,36-,37-,39+/m1/s1
  • Key:GOQPVIZMGXUXOL-GRLAPFOSSA-N

SRX251, orSRX-251, also known asAPI-251, is aselectivevasopressinV1A receptorantagonist that is or was under development for the treatment ofaggression.[1][3][4][2] It was also being developed for the treatment ofdysmenorrhea, but development for this indication was discontinued.[1] The drug is takenby mouth.[1][2] SRX251 reduces aggressive behavior in rodents.[4][2] It is or was being developed by Azevan Pharmaceuticals.[1][3] In 2007, it was inphase 1clinical trials.[1][3]

See also

[edit]

References

[edit]
  1. ^abcdef"SRX 251".AdisInsight. 3 January 2024. Retrieved24 February 2025.
  2. ^abcdFerris CF, Lu SF, Messenger T, Guillon CD, Heindel N, Miller M, et al. (February 2006). "Orally active vasopressin V1a receptor antagonist, SRX251, selectively blocks aggressive behavior".Pharmacology, Biochemistry, and Behavior.83 (2):169–174.doi:10.1016/j.pbb.2006.01.001.PMID 16504276.
  3. ^abc"Delving into the Latest Updates on SRX-251 with Synapse".Synapse. 22 February 2025. Retrieved24 February 2025.
  4. ^abMorrison TR, Melloni RH (2014). "The role of serotonin, vasopressin, and serotonin/vasopressin interactions in aggressive behavior".Current Topics in Behavioral Neurosciences.17:189–228.doi:10.1007/7854_2014_283.ISBN 978-3-662-44280-7.PMID 24496652.AVP is involved in various CNS circuits that underlie many different processes, including those related to the regulation of aggressive behavior, and various studies have used AVP agonists and antagonists to promote or block aggressive behaviors. For example, in resident male hamsters, oral administration of the V1A antagonist SRX251 reduces bite frequencies, and increases attack latencies during resident-intruder testing (Ferris et al. 2006).
Oxytocin
Vasopressin
V1A
V1B
V2
Unsorted
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