Membrane Transporters-Ion Channels

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  1. TRP agonist

    Evodiamine is a chemical extracted from the Tetradium family of plants. It acts primarily as a thermogenic and stimulant.
  2. Ca2+ channel agonist/CDK2 inhibitor

    Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
  3. TrpA1 channel agonist

    PF-4840154 is a non-electrophilic reference agonist of the TrpA1 channel. The TRPA1 channel is considered an attractive pain target based on the fact that TRPA1 knockout mice showed near complete attenuation of pain behaviors in some pre-clinical development models.
  4. glutamate receptors agonist

    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA).
  5. excitatory transmitter/agonist

    L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
  6. TRPM8 Agonist

    WS-12 is a potent TRPM8 agonist that acts as a cooling agent (EC50 = 193 nM).
  7. TRPM8 agonist

    WS 3 is TRPM8 receptors agonist (EC50 = 3.7 μM) and cooling agent.
  8. Peripheral chemoreceptor agonist

    Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel.
  9. TRPV1 agonist

    Zucapsaicin, also known as cis-Capsaicin, is a medication used to treat osteoarthritis of the knee and other neuropathic pain. It is applied three times daily for a maximum of three months. It reduces pain, and improves articular functions.
  10. TRPA1 agonist

    JT010 is a potent agonist of TRPA1 with an EC50 of 0.65 nM.
  11. kainate receptors agonist

    SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [3H]-kainate binding with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively.
  12. TRPV4 agonist

    RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM.
  13. TRPM8 agonist

    D-3263 is an agonist of transient receptor potential melastatin member 8 (TRPM8) with potential antineoplastic activity.
  14. L-type Ca2+ channel agonist

    (S)-(-)-Bay-K-8644 is an agonist of L-type Ca2+ channel. (S)-(-)-Bay-K-8644 activates Ba2+ currents (IBa) (EC50=32 nM).
  15. Piezo1 agonist

    Yoda 1 is a Piezo1 agonist. Yoda 1 activates purified Piezo1 channels.
  16. AMPAR agonist

    (S)-(-)-5-Fluorowillardiine is a potent and specific AMPAR agonist.
  17. AMPA/kainate receptors agonist

    (S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM.
  18. N- and P/Q-type Ca2+ channels agonist

    GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.
  19. OPRM1/OPRD1 agonist

    ML335 (CYM 51010, CID-23723457) is an agonist for OPRM1(μ-opioid receptor)-OPRD1(δ-opioid receptor) heterodimerization with EC50 of 403 nM demonstrating selectivity over the individual OPRM1 and OPRD1 receptors and the serotonin HT5A receptor with EC50 of 14.9 μM, 1.1 μM, and >40 μM, respectively.

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