Girisopam
Girisopam is a PDE inhibitor with IC50 values of 3.2, 4.0, and 12.5 μM against PDE4, PDE2, and PDE5, respectively. Girisopam exhibits anxiolytic, antidepressant, anti-aggressive, and antipsychotic activities. The binding sites of Girisopam are enriched exclusively in the basal ganglia of rat brains, and depletion of these sites is associated with damage to the striatonigral pathway. Girisopam enhances the potency of μ-opioid receptor agonists, attenuates the antagonistic effect of low-dose Naloxone (HY-17417A), and synergistically potentiates the anti-fighting effect of Chlorpromazine (HY-12708). Girisopam can be used in studies related to psychiatric disorders such as anxiety and depression.
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- No. CAS: 82230-53-3
- Fòrmula: C18H17ClN2O2
- Peso molecular:328.79
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Almacenamiento:
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Descripciòn
IC50 & Target
[1]|
PDE4 3.2 μM (IC50) |
PDE2 4.0 μM (IC50) |
PDE5 12.5 μM (IC50) |
In Vitro
Girisopam (compound 6a) inhibits purified PDE4 with an IC50 of 3.2 μM, and also exhibits activity against PDE2, PDE3, and PDE5 isoforms[1].
3H]girisopam (5 nM; 30 min) binds to sites concentrated in control rat striato-pallido-nigral brain regions, with measurable densities ranging from 31.5 to 44.4 nCi/mg, and binding is fully displaceable by 10-5 M unlabelled girisopam[2].
Girisopam binds to a specific site in rat striatal membrane preparations with a KD of 10.3 nM and a Bmax of 6.94 pmol/mg protein[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Girisopam (10 mg/kg; i.p.; single dose) synergistically enhances the anti-fighting effect of Chlorpromazine (HY-12708) in male CFLP mice[5].
Girisopam (50 mg/kg; i.p.; single administration) exerts no significant effect on chlorpromazine (HY-12708)-induced catalepsy in male Sprague-Dawley rats, and exhibits only extremely low catalepsy-inducing activity on its own[5].
Girisopam (50 mg/kg; i.p.; single administration) significantly enhances catalepsy induced by μ-opioid receptor agonists in male Sprague-Dawley rats, and attenuates the inhibitory effect of non-selective opioid receptor antagonists on this response[5].
Girisopam (10 mg/kg; i.p.; single administration) increases the analgesic potency of morphine by approximately 10-fold in the tail-flick test in male CFY/Harlem rats, attenuates the antagonistic effect of low-dose Naloxone (HY-17417A), and exhibits no analgesic activity itself[5].
Girisopam (20 mg/kg; intraperitoneal injection; single administration) significantly potentiates the inhibitory effect of Naloxone on sucrose intake in male Wistar rats, without affecting their water intake[5].
Girisopam (10 mg/kg; i.p.; single administration) does not alter the anticonvulsant effects of chlordiazepoxide against maximal electroshock-induced seizures and pentylenetetrazol-induced seizures in male CFLP mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CFLP (male, 18-22 g)[5]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Caused a significant decrease in mouse motility.
Inhibited μ-opioid receptor agonist-induced hypermotility, causing a rightward parallel shift of the μ-opioid receptor agonist dose-response curve.
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Animal Model:CFLP (male, 18-22 g)[5]
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Dosage:10 mg/kg; 7.75 mg/kg (ED50 for fighting inhibition alone)
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Administration:i.p.; single dose
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Result:Had an ED50 of 7.75 mg/kg for inhibiting fighting behavior.
Caused a significant leftward shift of the benzodiazepine sedative-hypnotic dose-response curve, indicating additive effects.
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Animal Model:Sprague-Dawley (male, 250-300 g)[5]
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Dosage:50 mg/kg
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Administration:i.p.; single dose
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Result:Produced a mean catalepsy score of 0.1.
Did not significantly modify chlorpromazine-induced catalepsy (no significant difference in scores compared to chlorpromazine-only groups via ANOVA and Kruskal-Wallis test).\nSignificantly augmented μ-opioid receptor agonist-induced catalepsy, increasing catalepsy scores across μ-opioid receptor agonist doses (10, 20, 30 mg/kg i.p.).
Reduced the inhibitory effect of non-selective opioid receptor antagonist on μ-opioid receptor agonist-induced catalepsy, with non-selective opioid receptor antagonist's antagonism much weaker in girisopam-pretreated rats.
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Animal Model:CFY/Harlem (male, 160-180 g)[5]
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Dosage:10 mg/kg; up to 80 mg/kg (no analgesia alone)
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Administration:i.p.; single dose
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Result:Did not induce analgesia up to 80 mg/kg i.p.
Increased morphine's analgesic potency ~10-fold, reducing morphine's ED50 from 0.87 mg/kg to 0.097 mg/kg.
Reduced the antagonistic effect of 1 mg/kg s.c. naloxone on morphine analgesia, though 3 mg/kg s.c. naloxone still shifted the morphine dose-response curve rightward.
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Animal Model:Wistar (Charles River, male, 240-260 g)[5]
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Dosage:20 mg/kg
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Administration:i.p.; single dose
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Result:Caused only a slight, non-significant decrease in sucrose consumption.
Augmented naloxone-induced inhibition of sucrose consumption.
Did not significantly alter water consumption.
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Animal Model:CFLP (male, 22-28 g)[5]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Did not alter the anticonvulsant activity of chlordiazepoxide, with chlordiazepoxide's ED50 remaining 32.4 mg/kg compared to 28.9 mg/kg for chlordiazepoxide alone.
Did not alter electroshock-induced seizures when administered alone.\nDid not alter the anticonvulsant activity of chlordiazepoxide, with chlordiazepoxide's ED50 remaining 1.36 mg/kg compared to 2.06 mg/kg for chlordiazepoxide alone.
Did not alter pentylenetetrazol-induced seizures when administered alone.
Chemical Information
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No. CAS 82230-53-3
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Peso molecular 328.79
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Fòrmula C18H17ClN2O2
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SMILES
ClC1=CC=CC(C2=NN=C(CC3=C2C=C(OC)C(OC)=C3)C)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Girisopam Related Classifications
HY-187129 Related Classifications
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