2. GPCR/G Protein
  3. Vasopressin Receptor
  4. Nelivaptan

Nelivaptan (SSR-149415) is a selective and orally active vasopressin V1b receptor antagonist (Ki: 3.7 and 1.3 nM for native and recombinant rat V1b receptors, respectively). Nelivaptan inhibits arginine vasopressin (AVP)-induced Ca2+ increase and corticotropin secretion. Nelivaptan can be used for research of stress, anxiety and depression.

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Nelivaptan Chemical Structure

Nelivaptan Chemical Structure

CAS No. : 439687-69-1

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Nelivaptan Related Antibodies

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Description

Nelivaptan (SSR-149415) is a selective and orally active vasopressin V1b receptor antagonist (Ki: 3.7 and 1.3 nM for native and recombinant rat V1b receptors, respectively). Nelivaptan inhibits arginine vasopressin (AVP)-induced Ca2+ increase and corticotropin secretion. Nelivaptan can be used for research of stress, anxiety and depression[1][2].

In Vitro

Nelivaptan (0.1-100 nM, 20 min) potently inhibits arginine vasopressin (AVP)-induced Ca2 increase in CHO cells transfected with the human V1b receptor[1].
Nelivaptan (0.9-15 nM, 45 min) inhibits [3H]AVP binding in a competitive manner in CHO cells transfected with the human V1b receptor[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Nelivaptan Related Antibodies
In Vivo

Nelivaptan (1-30 mg/kg; 30 min i.p. or 2 h p.o. before an exogenous AVP injection) inhibits exogenous AVP-induced increase in plasma corticotropin in Sprague-Dawley rats[1].
Nelivaptan (1-10 mg/kg; p.o.; 1, 2, 3, 4, and 6 h before the AVP challenge) produces powerful dose-dependent inhibition of the corticotropin increase in response to exogenous AVP plus corticotropin-releasing factor (CRF) in Sprague-Dawley rats[1].
Nelivaptan (1-10 mg/kg; i.p. 30 min or 60 min before test; or p.o. for 7 days) displays anxiolytic-like activity after acute and 7-day repeated administrations in male NMRI mice [1].
Nelivaptan (30 mg/kg; i.p.; daily for two weeks) retains efficacy in reducing both measured indices of depression-like behavior (learned helplessness and anhedonia), even when neurogenesis is blocked in male Wistar rats with chronic mild stress[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (300-400 g, aged 3 months) with chronic mild stress[2]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (i.p.); daily for two weeks
Result: Chronic administration reversed learned helplessness and anhedonia even when methylazoxymethanol (MAM) was administered.
Attenuated these depressive-like behaviors after 1 week.
Restored the density of Ki-67-positive cells to control levels.
Animal Model: Male Sprague-Dawley CD rats (275-300 g)[1]
Dosage: 1, 3, 10, 30 mg/kg
Administration: Intraperitoneal injection (i.p.) or Oral gavage (p.o.); 30 min i.p. or 2 h p.o. before an exogenous AVP injection
Result: Antagonized AVP-induced corticotropin secretion in a dose-dependent manner by both intraperitoneal and oral routes.
The inhibition was significant from 10 mg/kg p.o. and 3 mg/kg i.p. upwards.
The inhibitory action lasted significantly for more than 2 h at 10 mg/kg i.p. and up to 4 h at 10 mg/kg p.o..
Had no effect on basal corticotropin plasma levels up to 30 mg/kg p.o..
Animal Model: Male Sprague-Dawley CD rats (275-300 g)[1]
Dosage: 1, 3, 10 mg/kg
Administration: Oral gavage (p.o.); 1, 2, 3, 4, and 6 h before the AVP challenge (10 mg/kg)
Result: Produced powerful dose-dependent inhibition of the corticotropin increase in response to exogenous AVP plus corticoliberin; the effect was significant from the dose of 3 mg/kg p.o.. Complete blockade was achieved at 10 mg/kg.
Showed a fast onset of action, the inhibitory effect was maximal at 1 h after administration.
The inhibitory effect on corticotropin secretion lasted significantly more than 4 h, demonstrating a long-lasting oral effect in a specific V1b-related model.
Animal Model: Male NMRI mice (20 g)[1]
Dosage: 1, 3, 10 mg/kg
Administration: Intraperitoneal injection (i.p.) or Oral gavage (p.o.); i.p. (1, 3, 10 mg/kg) 30 min or 60 min befeore; p.o. (10 mg/kg) for 7 days,
Result: In the acute experiments, i.p. and p.o. compound increased the number of punished crossings showing marked anxiolytic effects.
Post hoc analysis revealed that these effects reached statistical significance from 3 mg/kg p.o. and i.p.
The anxiolytic-like activity was still significantly maintained when given repeatedly at 10 mg/kg p.o. for 7 days.
The oral time course of the anxiolytic-like action performed at 10 mg/kg indicated that effects lasted for more than 4 h.
Molecular Weight

630.11

Formula

C30H32ClN3O8S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(N(C(C=C1)=C2C=C1Cl)C([C@@]2(C3=CC=CC=C3OC)N4[C@@H](C[C@@H](O)C4)C(N(C)C)=O)=O)(C(C(OC)=C5)=CC=C5OC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (3.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5870 mL 7.9351 mL 15.8702 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5870 mL 7.9351 mL 15.8702 mL 39.6756 mL
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Nelivaptan Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nelivaptan439687-69-1SSR-149415SSR149415SSR 149415Vasopressin ReceptorcorticotropinstressanxietyCa2+arginine vasopressindepressionInhibitorinhibitorinhibit

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