8-Phenyltheophylline
Based on 1 Customer Validation
8-Phenyltheophylline is an adenosine receptor (adenosine receptor) antagonist. 8-Phenyltheophylline blocks adenosine-stimulated cAMP accumulation, inhibits tissue-selective cAMP hydrolysis, and antagonizes the inhibitory effects of adenosine. 8-Phenyltheophylline enhances apomorphine-induced rotational behavior in lesioned rats, reverses the analgesic effect of morphine in the rat hot plate test, and slightly enhances contractile responses of the atrium and ileum. 8-Phenyltheophylline can be used in studies related to unilateral nigrostriatal pathway injury.
For research use only. We do not sell to patients.
- CAS No.: 961-45-5
- Formula: C13H12N4O2
- Molecular Weight:256.26
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Adenosine Receptor Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
0.21 μM
Compound: 1
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Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
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[PMID: 11170626] |
| CHO-K1 | IC50 |
1.34 μM
Compound: 1
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Binding Affinity for Adenosine A1 receptor expressed in CHO-K1 cells compared to [3H]CCPA
Binding Affinity for Adenosine A1 receptor expressed in CHO-K1 cells compared to [3H]CCPA
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[PMID: 11170626] |
| Hepatocyte | IC50 |
1.1 μM
Compound: 1
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Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
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[PMID: 11170626] |
8-Phenyltheophylline (10 min) potently inhibits adenosine-stimulated cyclic AMP accumulation in rat hypothalamic slices, with a half-maximal inhibitory concentration (IC50) of approximately 1 μM[1].
8-Phenyltheophylline (0.5-25 μM) selectively inhibits cyclic nucleotide phosphodiesterase-mediated cAMP hydrolysis in rat erythrocytes and gastrocnemius muscles, and shows extremely low activity in rat adipocytes, abdominal aortas and brain extracts[2].
8-Phenyltheophylline (10 μM) potently and selectively inhibits the high-affinity cAMP phosphodiesterase isozyme in erythrocytes of *Rattus norvegicus* (inhibition rate: 55%)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
8-Phenyltheophylline (10 μg; intrathecal injection; single bolus administration) reverses morphine-induced analgesia in the hot-plate test but not in the tail-flick test in rats[3].
8-Phenyltheophylline (10 μg; intrathecal injection; single bolus) still reverses morphine-induced analgesia in the rat hot-plate test after degeneration of the noradrenergic descending pathway, but loses the ability to reverse morphine-induced antinociception in the rat hot-plate test after degeneration of the descending serotonergic pathway[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 160-180 g, unilateral nigro-striatal dopamine pathway lesion via stereotaxic injection of 8 μg 6-OHDA into left ventral tegmental area, selected for stable two-peak rotation pattern in response to apomorphine)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; single dose 30 minutes prior to apomorphine
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Result:Increased apomorphine-induced rotation to 108% of control.
Increased apomorphine-induced rotation to 127% of control.
Increased apomorphine-induced rotation to 133% of control.
Enhanced the trough between the two characteristic rotation peaks and augmented the second peak at the highest dose.
Did not stimulate rotation behaviour when administered alone.
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Animal Model:Sprague-Dawley (male, 325-350 g)[3]
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Dosage:10 μg
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Administration:i.t.; single bolus
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Result:Reversed morphine-induced antinociceptive action in the hot plate test.
Did not reverse morphine-induced antinociceptive action in the tail-flick test.
Showed no reversal in the hot plate test when morphine was administered at a 1.25 μg dose that produced minimal threshold increases.
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Animal Model:Sprague-Dawley (male, 325-350 g, descending noradrenergic pathway degeneration induced by intrathecal 6-OHDA)[3]
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Dosage:10 μg
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Administration:i.t.; single bolus
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Result:Reversed morphine-induced antinociception in the hot plate test in both vehicle-pretreated and 6-hydroxydopamine-pretreated rats.
Retained reversal ability even in a subgroup of rats with severe norepinephrine depletion.
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Animal Model:Sprague-Dawley (male, 325-350 g, descending serotonergic pathway degeneration induced by intrathecal 5,7-dihydroxytryptamine (HY-N18471) with Desipramine (HY-B1272A) pretreatment)[3]
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Dosage:10 μg
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Administration:i.t.; single bolus
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Result:Did not reverse morphine-induced antinociception in the hot plate test in rats pretreated with 5,7-dihydroxytryptamine.
Chemical Information
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CAS No. 961-45-5
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Appearance Solid
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Molecular Weight 256.26
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Formula C13H12N4O2
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SMILES
O=C(N1C)N(C)C2=C(N=C(C3=CC=CC=C3)N2)C1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
0.1 M NaOH : 1.67 mg/mL (6.52 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| 0.1 M NaOH | 1 mM | 3.9023 mL | 19.5114 mL | 39.0229 mL | 97.5572 mL |
| 5 mM | 0.7805 mL | 3.9023 mL | 7.8046 mL | 19.5114 mL |
8-Phenyltheophylline Related Classifications
HY-23133 Related Classifications
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