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Chemical Structure| 792173-99-0 Chemical Structure| 792173-99-0

Structure of SB-334867 free base
CAS No.: 792173-99-0

Chemical Structure| 792173-99-0

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SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with pKb of 7.2.

Synonyms: SB334867A free base; SB-334867

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Product Details of SB-334867 free base

CAS No. :792173-99-0
Formula : C17H13N5O2
M.W : 319.32
SMILES Code : O=C(NC1=CC=NC2=CC=CN=C12)NC3=CC=C4N=C(C)OC4=C3
Synonyms :
SB334867A free base; SB-334867
MDL No. :MFCD06411602
InChI Key :AKMNUCBQGHFICM-UHFFFAOYSA-N
Pubchem ID :6604926

Safety of SB-334867 free base

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315
Precautionary Statements:P280

Isoform Comparison

Biological Activity

Target
  • OX1 receptor

In Vitro:

Cell Line
Concentration Treated Time Description References
CeA neurons 10 μM SB-334867 significantly decreased sIPSC frequency in CeA neurons from LgA rats, indicating that HCRT-R1 regulates basal CeA GABA release in LgA rats. PMC5161745

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Cocaine self-administration model Intraperitoneal (systemic); Intra-CeA (intra-CeA) 0, 7.5, 15, 30 mg/kg (systemic); 0, 10, 20 nmol (intra-CeA) Single dose, 30 min prior (systemic); Single dose, 15 min prior (intra-CeA) Systemic SB-334867 dose-dependently reduced FR1 cocaine self-administration in LgA rats, and intra-CeA SB-334867 significantly reduced cocaine self-administration in LgA rats and attenuated stress-induced reinstatement of cocaine-seeking. PMC5161745
Mice Intracerebral hemorrhage model Intraperitoneal injection 10 mg/ml Once, 1 hour after ICH To study the neuroprotective mechanism of OXA, it was found that SB-334867 (OXR1 antagonist) had no significant effect on the anti-inflammatory effect of OXA PMC7294616
Sprague-Dawley rats Cocaine self-administration model Intracranial microinjection 1 mM Single injection, immediately before testing To investigate the effect of SB-334867 in VTA on cue-driven motivation for cocaine. Results showed that SB-334867 reduced motivation only when animals were exposed to cocaine-associated cues during training and testing. PMC8782853
Mice Morphine-induced sensitization to locomotor activity model Intraperitoneal injection 20 mg/kg Administered 15 min before morphine injection, 5 times, with 3-day intervals SB-334867 inhibited the acquisition of morphine-induced sensitization to locomotor activity and significantly altered the mRNA expression of orexin, dopamine, and adenosine receptors, as well as the expression of GFAP and Iba-1 in the brain. PMC6153720
Rats Fentanyl self-administration model Intraperitoneal injection 3, 10, or 30 mg/kg Administered 30 min prior to testing, with a minimum of 3 days between tests SB-334867 increased demand elasticity (decreased motivation) for fentanyl without affecting consumption at null cost. Baseline α values predicted SB efficacy, with SB being most effective in highly motivated animals. SB also attenuated cue-induced reinstatement of fentanyl seeking. PMC6785092
Mice Alcohol dependence model Intraperitoneal injection 3 mg/kg Once daily, for 2 hours OX1R signaling plays a particular role in promoting compulsive-like alcohol drinking, and low doses of SB-334867 significantly reduced compulsive-like alcohol consumption PMC5065938
Mice Restraint stress model Intraperitoneal injection 15 mg/kg Single injection, lasting 30 minutes To investigate the effect of SB-334867 on restraint stress-induced analgesia, results showed that SB-334867 significantly inhibited the restraint stress-induced analgesia. PMC8081448
Rats Adult male Sprague Dawley rats Intraperitoneal injection 1 mg/kg Single dose To assess the effect of SB-334867 on the hypoxic ventilatory response, results showed that SB-334867 significantly reduced the hypoxic ventilatory response. PMC11223477

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.13mL

0.63mL

0.31mL

15.66mL

3.13mL

1.57mL

31.32mL

6.26mL

3.13mL

References

 

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