SRX251

SRX251
Clinical data
Other names	SRX-251; API-251; API251
Routes of; administration	Oral
Drug class	Vasopressin V1A receptor antagonist
Identifiers
	IUPAC name (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	512784-94-0;
PubChem CID	11686429;
ChemSpider	9861157;
UNII	G9Z22EU5FK;
ChEMBL	ChEMBL279328;
Chemical and physical data
Formula	C43H48F3N5O5
Molar mass	771.882 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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, or SRX-251, also known as API-251, is a selective vasopressin V_1A receptor antagonist that is or was under development for the treatment of aggression.^[1]^[3]^[4]^[2] It was also being developed for the treatment of dysmenorrhea, but development for this indication was discontinued.^[1] The drug is taken by 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 in phase 1 clinical trials.^[1]^[3]

References

^ ^a ^b ^c ^d ^e ^f "SRX 251". AdisInsight. 3 January 2024. Retrieved 24 February 2025.
^ ^a ^b ^c ^d Ferris 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.
^ ^a ^b ^c "Delving into the Latest Updates on SRX-251 with Synapse". Synapse. 22 February 2025. Retrieved 24 February 2025.
^ ^a ^b Morrison 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).

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