OPC 31260 hydrochloride - CAS 138470-70-9
Catalog number: 138470-70-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Vasopressin Receptor
OPC 31260 is a Vasopressin receptor antagonist marketed by Otsuka. It is a benzazepine derivative that antagonizes the binding of arginine vasopressin (AVP) to vasopressin receptors located in the liver (V1; IC50 = 1.2 µM) and kidney (V2; IC50 = 14 nM). In Japan, OPC 31260 was approved in October 2006 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH) due to ADH producing tumors.
Publictions citing BOC Sciences Products
  • >> More
white to tan powder
N-(4-(5-(dimethylamino)-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)phenyl)-2-methylbenzamide hydrochloride;OPC31260;
Soluble in DMSO
-20°C Freezer
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
Current Developer:
Originator Otsuka Pharmaceutical
1.Acute aquaresis by the nonpeptide arginine vasopressin (AVP) antagonist OPC-31260 improves hyponatremia in patients with syndrome of inappropriate secretion of antidiuretic hormone (SIADH).
Saito T1, Ishikawa S, Abe K, Kamoi K, Yamada K, Shimizu K, Saruta T, Yoshida S. J Clin Endocrinol Metab. 1997 Apr;82(4):1054-7.
The present study was undertaken to determine whether the non-peptide V2 arginine vasopressin (AVP) antagonist 5-dimethylamino- 1[4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepi ne hydrochloride (OPC-31260) produces water diuresis and improves hyponatremia in patients with the syndrome of inappropriate secretion of antidiuretic hormone (SIADH). Eleven patients (9 males and 2 females, 64 +/- 3.5 yr) with SIADH were included in the present protocol, which was comprised of 3 successive days. Day 1 was a control day, and on days 2 and 3 OPC-31260 was administered intravenously. Five blood and urine collections were made at 1-2 h intervals during the 6 h observation period each day. A single administration of 0.25 and 0.5 mg/kg OPC-31260 increased the 4 h cumulative urine volume and decreased urinary osmolality to below 225 mOsm/kg H2O. Such a diuretic effect was independent of an increase in urinary solute excretions. This aquaresis by 0.
2.Clinical implication of the antidiuretic hormone (ADH) receptor antagonist mozavaptan hydrochloride in patients with ectopic ADH syndrome.
Ectopic ADH Syndrome Therapeutic Research Group1, Yamaguchi K, Shijubo N, Kodama T, Mori K, Sugiura T, Kuriyama T, Kawahara M, Shinkai T, Iguchi H, Sakurai M. Jpn J Clin Oncol. 2011 Jan;41(1):148-52. doi: 10.1093/jjco/hyq170. Epub 2010 Nov 17.
Ectopic antidiuretic hormone syndrome is a medical emergency characterized by dilutional hyponatremia. Clinical effectiveness of the vasopressin V2 receptor antagonist mozavaptan was evaluated in 16 patients. In short-term (7-day) treatment with the drug, serum sodium concentration (mean ± standard deviation) significantly (P = 0.002) increased from 122.8 ± 6.7 to 133.3 ± 8.3 mEq/l, and symptoms due to hyponatremia were improved. On the basis of these results, mozavaptan (Physuline(®)) was approved as an orphan drug for the treatment of the syndrome in 2006 in Japan. During the 43 months following its launch, 100 patients have been treated with the drug; overall clinical effects of the drug were found similar to those of this clinical trial. Clinically, mozavaptan may allow hyponatremic patients to be treated by aggressive cancer chemotherapy with platinum-containing drugs. Moreover, the drug may free patients from strict fluid-intake restrictions and thereby improve their quality of life.
3.Vasopressin receptor antagonist OPC-31260 prevents cerebral oedema after subarachnoid haemorrhage.
László FA1, Varga C, Nakamura S. Eur J Pharmacol. 1999 Jan 8;364(2-3):115-22.
The effects of the non-peptide vasopressin V2 receptor antagonist, 5-dimethylamino-1-[4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrah ydro-1 H-benzazepine hydrochloride (OPC-31260) on the cerebral oedema induced by subarachnoid haemorrhage were studied in rats. Subarachnoid haemorrhage induced significant water retention after water loading, increased the brain content of water and Na+ and increased plasma vasopressin levels. The water retention and brain water and Na+ accumulation were prevented by OPC-31260 administration, but the plasma vasopressin levels were further enhanced by OPC-31260. These results demonstrate the important role of vasopressin in the development of antidiuresis and disturbances in brain water and electrolyte balance in response to subarachnoid haemorrhage. The subarachnoid haemorrhage-induced cerebral oedema was significantly reduced following oral OPC-31260 administration. The protective mechanism exerted by OPC-31260 stems from its influence on renal tubular function: it blocks the renal vasopressin V2 receptors.
4.Prevention of hypoxic brain oedema by the administration of vasopressin receptor antagonist OPC-31260.
Molnár AH1, Varga C, Berkó A, Rojik I, Párducz A, László F, László FA. Prog Brain Res. 2008;170:519-25. doi: 10.1016/S0079-6123(08)00439-1.
The numerous situations which can result in cerebral hypoxic damage occur in newborn infants and in the elderly. In research aimed at more effective therapeutic intervention in ischaemic disorders of the brain, the animal model used and the principles of the causal therapy should be better outlined. The effects of the non-peptide AVPR (V2) antagonist 5-dimethylamino-1-[4-(2-methylbenzoylamino) benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine hydrochloride (OPC-31260) on the cerebral oedema induced by general cerebral hypoxia were studied in rats. The general cerebral hypoxia was produced by bilateral common carotid ligation in Sprague-Dawley rats of the CFY strain. By 6h after the ligation, half of the rats had died, but the survival rate was significantly higher following OPC-31260 administration. Electron microscopic examinations revealed typical ischaemic changes after the carotid ligation, and OPC-31260 treatment did not significantly reduce the hypoxic signs in the brain cortex; only a certain decrease in the pericapillary oedema was observed.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Vasopressin Receptor Products

CAS 347887-36-9 Fedovapagon

(CAS: 347887-36-9)

Fedovapagon is a potent, nonpeptidic vasopressin V2 receptor agonists (EC50 of 24 nM), demonstrated positive anti-diuretic effect in nocturia

CAS 138470-70-9 OPC 31260 hydrochloride

OPC 31260 hydrochloride
(CAS: 138470-70-9)

OPC 31260 is a Vasopressin receptor antagonist marketed by Otsuka. It is a benzazepine derivative that antagonizes the binding of arginine vasopressin (AVP) to ...

CAS 1642187-96-9 TASP 0390325

TASP 0390325
(CAS: 1642187-96-9)

TASP 0390325 is a potent and selective vasopressin V1B receptor antagonist (IC50 = 2.22 nM for rat pituitary receptor) with no significant affinity for 85 other...

CAS 210101-16-9 Conivaptan

(CAS: 210101-16-9)

Conivaptan, also called as YM 087 or Vaprisol, is the first is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist) approved by Un...

CAS 56-59-7 Felypressin

(CAS: 56-59-7)

Felypressin is a Vasopressin 1 agonist and has effects at all Arginine vasopressin receptor 1As. It is a non-catecholamine vasoconstrictor that is chemically re...

CAS 42061-33-6 d[leu4,Lys8]-VP

(CAS: 42061-33-6)

d[leu4,Lys8]-VP is a selective vasopressin V1B receptor agonist (Ki = 0.16, 64, 100 and 3800 nM for V1B, oxytocin, V2 and V1A receptors, respectively). It exhib...

CAS 150683-30-0 Tolvaptan

(CAS: 150683-30-0)

Tolvaptan is an orally effective nonpeptide arginine vasopressin V2 receptor antagonist with IC50 of 3 nM, used to treat hyponatremia.

CAS 62288-83-9 Desmopressin Acetate

Desmopressin Acetate
(CAS: 62288-83-9)

Desmopressin acetate, a syntheticpeptide containing nine amino acids, is analogue of the antidiuretic hormone arginine vasopressin. Improves hemostatsis by incr...

CAS 479232-57-0 TC OT 39

TC OT 39
(CAS: 479232-57-0)

TC OT 39 is a potent non-peptide oxytocin receptor partial agonist (EC50 = 33 nM and 850 nM for the oxytocin receptor and V2 vasopressin receptor, respectively)...

CAS 909391-88-4 Vasopressin antagonist 1867

Vasopressin antagonist 1867
(CAS: 909391-88-4)

Vasopressin antagonist 1867 is a selective vasopressin 1B (V1b) receptor antagonist (IC50 value 3 nM for hV1b inhibition, exhibiting >1000-fold selectivity over...

CAS 168079-32-1 VPA-985

(CAS: 168079-32-1)

VPA-985, an azepine compound, has been found to be a Vasopressin receptor antagonist that could be used in some cardiovascular disease therapy like hyponatraemi...

(CAS: 1245620-47-6)

Ribuvaptan is a vasopressin receptor antagonist originated by Bayer HealthCare Pharmaceuticals. Now, Ribuvaptan is still in phase I development for the treatmen...

CAS 168626-94-6 Conivaptan HCl

Conivaptan HCl
(CAS: 168626-94-6)

Conivaptan HCl is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist).

CAS 500170-27-4 d[Cha4]-AVP

(CAS: 500170-27-4)

d[Cha4]-AVP is a selective and potent human vasopressin V1B receptor agonist with Ki value of 1.2 nM. It stimulates corticosterone and ACTH secretion. It shows ...

CAS 113-79-1 Argipressine

(CAS: 113-79-1)

This molecular is a polypeptide which is a Antidiuretic hormone that has been found in most mammalian species and it acts as a neurotransmitter at synapses in t...

CAS 16679-58-6 Desmopressin

(CAS: 16679-58-6)

Desmopressin, a synthetic analog of the endogenous antidiuretic hormone arginine vasopressin with low vasopressor activity, is a dual antagonist of V1B and V2 r...

CAS 439687-69-1 SSR 149415

SSR 149415
(CAS: 439687-69-1)

SSR 149415 is a potent and orally available vasopressin V1B antagonist (Ki = 3.7 and 1.3 nM for native and recombinant rat V1b receptors, respectively), display...

CAS 131631-89-5 OPC 21268

OPC 21268
(CAS: 131631-89-5)

OPC-21268 is a vasopressin V1 receptor antagonist with IC50 value of 0.4 μM.

Chemical Structure

CAS 138470-70-9 OPC 31260 hydrochloride

Quick Inquiry

Verification code

Featured Items