vasopressin v1a receptor

L-371,257 is a competitive antagonist of oxytocin receptor with pA2 of 8.4 and Ki of 19 nM. L-371,257 shows a Ki of 3.7 nM for vasopressin receptor 1a.

LIT-001 improves social interaction in a mouse model of autism.It is the first nonpeptide oxytocin receptor agonist with EC50 of 55 nM and Ki of 226 nM.

SRX246 has no interaction at V1b and V2 receptors. SRX246 shows negligible binding at 64 other receptors classes, including 35 G-proteincoupled receptors. SRX246 is a potent and CNS-penetrant vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V

VNA-932 is an agonist of the vasopressin V2-receptor (IC50: 80.3 nM and 778 nM in human-V2 binding and V1a binding assay).

Conivaptan, a non-peptide inhibitor of antidiuretic hormone, was approved for hyponatremia caused by the syndrome of inappropriate antidiuretic hormone (SIADH), there is also some evidence that it may be effective in heart failure. Conivaptan inhibits sub

vasopressin V1A receptor antagonist

L-368899 is a non-peptide and orally active antagonist of oxytocin receptor (IC50: 8.9 nM). It displays 40-fold selectivity over vasopressin V1a and V2 receptors (IC50: 370 and 570 nM respectively).

RWJ 676070 is an antagonist of vasopressin V1A/V2 receptor.

Selepressin, an analog of vasopressin, is a potent, selective vasopressin V1a receptor agonist.

SRX 251, a vasopressin V1a receptor antagonist, is used potentially for the treatment of primary dysmenorrhea.

YM 218 is a novel, potent, selective antagonist of nonpeptide vasopressin V1A receptor.

YM 471 is a non-peptide arginine vasopressin (AVP) V1A and V2 receptor antagonist with oral activity.

Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.

d[Cha4]-AVP TFA is a potent and selective agonist for the vasopressin (AVP) V1b receptor, with a high affinity (K i of 1.2 nM). It shows greater selectivity for the V1b receptor over the V1a receptor, V2 receptor, and oxytocin receptors, demonstrating specificity in targeting the human V1b receptor [1] [2].

Val9-Oxytocin, an Oxytocin analog where Gly9 is substituted with Val9 [1], functions as a complete antagonist of the vasopressin (V1a) receptor.

(d(CH2)5[Tyr(Me)2, Dab5]AVP), a vasopressin V1a receptor-specific antagonist, demonstrates a pA2 value of 6.71 [1].

Invopressin (Compound 42), a vasopressin V1A receptor partial agonist (EC50: 1.0 nM), is utilized in research related to cirrhosis conditions such as bacterial peritonitis, HRS2, and refractory ascites [1].

Endolide F (Compound 2) is a proline-containing lactone that serves as a moderate antagonist of the arginine vasopressin V1A receptor.

Selective vasopressin V1B receptor agonist (Ki values are 0.16, 64, 100 and 3800 nM for V1B, oxytocin, V2 and V1A receptors respectively). Displays weak antidiuretic, vasopressor and in vitro oxytocic activities.

Potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). Stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.

d[Cha4]-AVP acetate is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). Stimulates ACTH and corticosterone secretion and exhibits negligible vasopr

Selective vasopressin V1A receptor antagonist. Inhibits vasopressin and oxytocin-induced increases in intracellular calcium concentrations in vitro (IC50 values are 5 and 30 nM respectively). Exhibits potent and prolonged antivasopressor activity and indu