PAM-2
PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC50: 39 μM, rat α7 nAChR EC50: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC50 = 174 μM) and CaV2.2 channel (IC50 = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic pain.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 1426293-61-9
- Fòrmula: C14H13NO2
- Peso molecular:227.26
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas Calcium Channel
More
Actividad biológica
|
human α7 nAChR 39 μM (EC50) |
rat α7 nAChR 12 μM (EC50) |
CaV2.2 89 μM (IC50) |
α9α10 nAChR 174 μM (IC50) |
PAM-2 (0.3 μM-1 mM; 5 min) potentiates Ach (30 μM)-activated α7 nAChRs in Xenopus oocytes in a concentration-dependent manner[1].
PAM-2 (0.3 μM-1 mM; 2 min) inhibits ACh (10 μM)-evoked currents at rα9α10 nAChRs in Xenopus oocytes in a concentration-dependent and voltage-independent manner[1].
PAM-2 (0.3 μM-1 mM) inhibits Cav2.2 channel-mediated Ba2+ currents without affacting G protein-coupled GABABR in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PAM-2 (1 mg/kg; p.o; coadministered with Oxaliplatin schedule for 14 days; and an extra dose 30 min post last co-treatment) prevents pain establishment when combined with Oxaliplatin, and increases pain threshold in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male CD-1 albino mice (2-3 months old) intraperitonealy injected with STZ (100 mg/kg)[1]
-
Dosage:1, 3 mg/kg
-
Administration:p.o.; single dose on day 15 post-STZ
-
Result:Significantly decreased neuropathic pain between 15 and 45 min at 3 mg/kg, 45 min, with complete reversal at 30 min.
Showed no effect at 1 mg/kg.
-
Animal Model:Male CD-1 albino mice (2-3 months old) intraperitonealy injected with Oxaliplatin (2.4 mg/kg) on days 1-3, 6-10, and 13-14[1]
-
Dosage:1, 3 mg/kg
-
Administration:p.o.; single dose on day 15 post-Oxaliplatin
-
Result:Significantly decreased neuropathic pain from 15 to 45 minutes after administration, with peak reversal at 30 min at 3 mg/kg.
Showed no effect at 1 mg/kg.
-
Animal Model:Male CD-1 albino mice (2-3 months old) intraperitonealy injected with Oxaliplatin (2.4 mg/kg) on days 1-3, 6-10, and 13-14[1]
-
Dosage:1 mg/kg
-
Administration:p.o; coadministered with oxaliplatin schedule for 14 days; and an extra dose 30 min post last co-treatment
-
Result:Prevented pain establishment by day 14.
An additional administration on the test day produced greater pain reversal within 0-30 min.
Chemical Information
-
No. CAS 1426293-61-9
-
Peso molecular 227.26
-
Fòrmula C14H13NO2
-
SMILES
N(C(/C=C/C1=CC=CO1)=O)C2=CC=C(C)C=C2
-
Envío
Room temperature in continental US; may vary elsewhere.
-
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)
PAM-2 Related Classifications
HY-180400 Related Classifications
Powered by Bioz