113158-34-2
113158-34-2 structure
- Name: Norbinaltorphimine dihydrochloride
- Chemical Name: Norbinaltorphimine dihydrochloride
- CAS Number: 113158-34-2
- Molecular Formula: C40H45Cl2N3O6
- Molecular Weight: 734.71
- Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
- Create Date: 2018-05-10 17:11:18
- Modify Date: 2024-01-12 15:44:02
-
Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
| Name | Norbinaltorphimine dihydrochloride |
|---|
| Description | Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist. |
|---|---|
| Related Catalog | |
| Target |
κ opioid receptor[1] |
| In Vitro | Norbinaltorphimine reversibly antagonize the effects of κ agonists with pA2 values of 10.2-10.4. Norbinaltorphimine is much less potent as an antagonist at μ and δ receptors, pA2 values are 7.4-7.6 and 7.6-7.8, respectively[1]. |
| In Vivo | Norbinaltorphimine has weak and inconsistent effects on THC-induced taste avoidance in adolescent rats in that Norbinaltorphimine both attenuates and strengthens taste avoidance dependent on dose and trial. Norbinaltorphimine has limited impact on the final one-bottle avoidance and no effects on the two-bottle preference test. Interestingly, Norbinaltorphimine has no effect on THC-induced taste avoidance in adult rats as well[2]. Norbinaltorphimine pretreatment significantly attenuates stress-induced reinstatement of nicotine-CPP, but has no effect on nicotine-primed reinstatement[3]. |
| Animal Admin | Rats[2] Norbinaltorphimine is dissolved in sterile H2O at a concentration of 15 mg/mL and administered subcutaneously (SC) at a dose of 15 mg/kg. Male Sprague Dawley rats are ranked according to average water consumption on all habituation cycles and assigned to one of two groups [Norbinaltorphimine (n=42) and Vehicle (n=42)], such that mean water intake is comparable among groups. On PND 34 (approximately 24 h prior to conditioning, see below), subjects assigned to the Norbinaltorphimine group are injected with Norbinaltorphimine (15 mg/kg) and subjects assigned to the Vehicle group are injected with the Norbinaltorphimine vehicle at an equal volume[2]. Mice[3] Mice are conditioned with 0.5 mg/kg nicotine, injected subcutaneously (s.c.) for 3 days and tested in the nicotine-conditioned place preference (CPP) model. After 3 days extinction, Norbinaltorphimine (10 mg/kg, s.c.) is administered 16 h prior to a priming dose of nicotine (0.1 mg/kg, s.c.), and mice are tested in the CPP model for nicotine-induced reinstatement of CPP. A separate group of mice is subjected to a 2-day modified forced swim test (FST) paradigm to induce stress after 3 days extinction from CPP. Mice are given vehicle or Norbinaltorphimine (10 mg/kg, s.c.) 16 h prior to each FST session[3]. |
| References |
| Molecular Formula | C40H45Cl2N3O6 |
|---|---|
| Molecular Weight | 734.71 |