| Name | Nelivaptan |
| Description | Nelivaptan (SR 149415) is a vasopressin V1b receptor antagonist that can eliminate CHS-induced GE damage and inhibit [3H]AVP binding in a competitive manner. |
| In vitro | METHODS: Nelivaptan (SR 149415) (1.25 nM, 2.5 nM and 5 nM) was used to treat In-R1-G9 pancreatic model cells, and the inhibitory effect of Nelivaptan on the specific binding of [3H]AVP (radiolabeled vasopressin) was detected.
RESULTS As the concentration of Nelivaptan5 increased, the Kd value (dissociation constant) under control conditions showed a dose-dependent decrease, which indicated that Nelivaptan inhibited the binding of [3H]AVP in a competitive manner, and the Ki value of Nelivaptan (inhibition constant) is 1.61 ± 0.17 nM. [1] |
| In vivo | METHODS: Animals in the male Wistar rat administration group and the Nelivaptan (SR 149415) group were intraperitoneally injected with drug (1ml/kg, 5% DMSO, 95% normal saline) or Nelivaptan dissolved in the drug (1ml/kg; stock solution concentration 5mg/kg) , the rats were placed in a high temperature environment of 38°C for 60 minutes, and the body weight and rectal temperature were measured before and immediately after treatment.
RESULTS Nelivaptan treatment reduced intracranial V1bR levels. [2]
METHODS: Nelivaptan was injected with DMSO as solvent at a dose of 1 nmol/rat (icv) with a volume of 5µl. The rats were monitored under basal non-stress (NS) conditions, acute stress (AS), CHS and CHeS. Changes in hypothalamic OXT and AVP release under conditions.
RESULTS Nelivaptan could eliminate CHS-induced GE damage. [3] |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (79.35 mM)
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| Keywords | Nelivaptan | SSR 149415 | SR149415 | SSR-149415 |
| Inhibitors Related | Atosiban acetate | Desmopressin acetate (16679-58-6 free base) | OPC-51803 | Felypressin acetate | Balovaptan | d[Cha4]-AVP acetate(500170-27-4 free base) | TASP0390325 | d[Leu4,Lys8]-VP acetate | L-371,257 | Fuscoside | Conopressin S acetate(111317-90-9 free base) | Tolvaptan |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
