2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR Calcium Channel
  4. 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.

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PAM-2

PAM-2 Chemical Structure

CAS No. : 1426293-61-9

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PAM-2 Related Antibodies

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Description

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[1].

IC50 & Target[1]

human α7 nAChR

39 μM (EC50)

rat α7 nAChR

12 μM (EC50)

CaV2.2

89 μM (IC50)

α9α10 nAChR

174 μM (IC50)

In Vitro

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 Related Antibodies
In Vivo

PAM-2 (1 and 3 mg/kg; p.o.; single dose on day 15 post-STZ) reduces STZ and Oxaliplatin-induced neuropathic pain in mice[1].
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.
Molecular Weight

227.26

Formula

C14H13NO2
CAS No.
SMILES

N(C(/C=C/C1=CC=CO1)=O)C2=CC=C(C)C=C2
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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PAM-2 Related Classifications

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Help & FAQs
  • 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:

PAM-21426293-61-9PAM2PAM 2nAChRCalcium ChannelNicotinic acetylcholine receptorsCa2+ channelsCa channelshuman α7 nAChRsCD-1 albino micerat α7 nAChRshCa_V2.2 channelsoxaliplatin-induced neuropathic painSTZ-induced neuropathic painα7 nicotinic acetylcholine receptoranti-nociceptive pain activityα7 nAChRrα9α10 nAChRsInhibitorinhibitorinhibit

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