2. GPCR/G Protein Neuronal Signaling PI3K/Akt/mTOR
  3. Opioid Receptor mTOR
  4. PF-04455242

PF-04455242 is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-04455242 blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-04455242 promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-04455242 attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-04455242 can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal.

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PF-04455242

PF-04455242 Chemical Structure

CAS No. : 1202647-54-8

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PF-04455242 Related Antibodies

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

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mTOR mTORC1 mTORC2

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Description

PF-04455242 is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-04455242 blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-04455242 promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-04455242 attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-04455242 can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal[1][2][3][4].

IC50 & Target[2]

human κ-opioid receptor (hKOR)

3.0 nM (Ki)

In Vitro

PF-04455242 (100 nM-1 μM) is a partial κ-opioid receptor antagonist with an IC50 of 6.7 nM in dopamine neurons of the rat ventral tegmental area (VTA); at concentrations of 100 nM and 1 μM, it induces outward K+ currents in a subset of these neurons[2].
PF-04455242 (60 minutes at room temperature) binds with high affinity (Ki = 3 nM) to human KOR stably expressed in CHO cells, and also binds with high affinity to rat KOR stably expressed in CHO cells (Ki = 21 nM) as well as mouse primary forebrain KOR (Ki = 22 nM)[4].
PF-04455242 (treated at 30°C for 20 min; treated at 30°C for 30 min) acts as an antagonist of human KOR stably expressed in CHO cells, with higher potency (Ki = 1.2 nM) than that against human MOR (Ki = 10 nM)[4].

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

PF-04455242 Related Antibodies
In Vivo

PF-04455242 (3.4 nM/day; i.c.v.; continuous infusion; 7 days) reduces body weight gain in ovariectomized wild-type female mice, an effect independent of food intake, accompanied by upregulated expression of thermogenic markers in adipose tissue and activation of the hypothalamic mTOR signaling pathway[3].
PF-04455242 (0.32-10 mg/kg; s.c.; single dose; 1 h before agonist administration) dose-dependently blocks the analgesic effects induced by KOR and MOR agonists in rats, and achieves dose-dependent, time-limited target binding to KOR and MOR in rat brains[4].
PF-04455242 (0.32-10 mg/kg; s.c.n; single administration; 30 minutes prior to Spiradoline treatment) dose-dependently blocks Spiradoline (HY-106756)-induced elevation of plasma prolactin in rats, with an ED50 of 2.3 mg/kg[4].
PF-04455242 (0.32-10 mg/kg; s.c.; single administration; 1 h before testing) exhibits antidepressant-like efficacy in the mouse forced swim test, alleviates depression-like social defeat behavior in mice following repeated stress exposure, and prevents stress-induced reinstatement of extinguished cocaine-seeking behavior in mice[4].

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

Animal Model: C57BL/6 wild-type (female, 8-10 weeks old, ovariectomy-induced obesity)[3]
Dosage: 3.4 nM/day
Administration: i.c.v.; continuous infusion; 7 days
Result: Significantly reduced cumulative body weight gain compared to vehicle control (p < 0.05).
Showed no change in cumulative food intake.
Demonstrated a non-significant tendency toward reduced subcutaneous inguinal white adipose tissue depots (p = 0.07).
Significantly increased uncoupling protein 1-positive immunostaining in brown adipose tissue (p < 0.05) and subcutaneous inguinal white adipose tissue (p < 0.05) compared to vehicle control.
Significantly increased phosphorylated levels of mTOR (pmTOR) and phosphorylated S6 (pS6) in the medio-basal hypothalamic area (p < 0.01).
Showed a non-significant tendency toward increased phosphorylated p70S6K (pS6K) levels in the medio-basal hypothalamic area (p = 0.06).
Animal Model: Sprague-Dawley (male, 175-200 g); Sprague-Dawley (male, jugular vein cannulated, 300-400 g)[4]
Dosage: 0.32, 1, 3.2, 10, 17.8, 32 mg/kg/0.1, 1, 3.2, 10, 32 mg/kg; 10 mg/kg (time-course)
Administration: s.c.; single dose; 1 hour before agonist administration
Result: Attenuated Spiradoline-induced tail-flick latency with an EC50 of 1.5 mg/kg.
Attenuated Morphine-induced tail-flick latency with an EC50 of 9.8 mg/kg.
Inhibited ex vivo [3H]CI977 binding to KORs with an ID50 of 2.0 mg/kg.
Inhibited ex vivo [3H]DAMGO binding to MORs with an ID50 of 8.6 mg/kg.
At 10 mg/kg, inhibited ex vivo [3H]CI977 binding by 60% at 15 minutes post-dose, reached maximal 82% inhibition at 30 minutes, maintained inhibition for 2 h, and showed no inhibition by 8 hours.
Inhibited in vivo [3H]PF-04767135 binding to KORs with an ID50 of 5.2 mg/kg.
Animal Model: Sprague-Dawley (male, jugular vein cannulated, 300-400 g)[4]
Dosage: 0.32, 1, 3.2, 10 mg/kg
Administration: s.c.; single dose; 30 minutes before spiradoline
Result: Dose-dependently reduced Spiradoline-induced plasma prolactin elevation with an ED50 of 2.3 mg/kg.
At 3.2 or 10 mg/kg, had no effect on basal prolactin levels.
Animal Model: ICR (male, 25-30 g)[4]
Dosage: 0.32, 1, 3.2 mg/kg/1, 3, 10 mg/kg
Administration: s.c.; single dose; 1 hour before testing/s.c.; daily; 3 days, 30 minutes before each social defeat trial
Result: Reduced immobility with a minimal effective dose of 3.2 mg/kg.
Dose-dependently reduced time spent in defeated postures: the 3 mg/kg dose produced a significant reduction on day 2, and all three doses produced significant reductions on day 3.
Clinical Trial
Molecular Weight

372.52

Formula

C21H28N2O2S
CAS No.
SMILES

O=S(C1=CC=CC=C1C2=CC=C(CNCC(C)C)C=C2)(N3CCCC3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PF-04455242 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:

PF-044552421202647-54-8PF04455242PF 04455242Opioid ReceptormTORMammalian target of Rapamycinδ-opioid receptorswhite adipose tissueHEK293 cellsventral tegmental area neuronshypothalamic mTOR pathwayKappa opioid receptorbrown adipose tissueμ-opioid receptorCHO cellsrat VTA dopamine neuronsInhibitorinhibitorinhibit

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