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 ǰȳ  Ű   Pharmacology

AMPA and Kainate Receptors Small molecules

AMPA and Kainate Receptors ʿ Small molecules Ұմϴ.

TOCRIS
ǰ ϱ
μϱ




Agonist
Cat. No. Product Name / Activity
1074 (RS)-AMPA hydrobromide
Selective AMPA agonist; more water soluble form of (RS)-AMPA (Cat. No. 0169)
0253 (R)-AMPA
Inactive isomer of (RS)-AMPA (Cat. No. 0169)
0169 (RS)-AMPA
Selective AMPA agonist
0254 (S)-AMPA
Selective AMPA agonist; active isomer of (RS)-AMPA (Cat. No. 0169)
1673 Cl-HIBO
GluA1 and GluA2 selective AMPA agonist
1543 (S)-CPW 399
Subtype-selective weakly desensitizing AMPA agonist
3840 NPEC-caged-(S)-AMPA
Caged (S)-AMPA
0188 L-Quisqualic acid
AMPA agonist; also group I mGlu agonist
Antagonist
Cat. No. Product Name / Activity
1082 CFM-2
Non-competitive AMPA antagonist
0190 CNQX
Potent and selective non-NMDA iGluR antagonist
1045 CNQX disodium salt
Potent non-NMDA iGluR antagonist; more water soluble form of CNQX (Cat. No. 0190)
2932 CP 465022 hydrochloride
Selective and non-competitive AMPA antagonist
0189 DNQX
Selective non-NMDA iGluR antagonist
2312 DNQX disodium salt
Selective non-NMDA iGluR antagonist; water-soluble salt of DNQX (Cat. No. 0189)
0845 Evans Blue tetrasodium salt
Non-NMDA iGluR antagonist; P2X antagonist; also inhibits L-glutamate uptake into synaptic vesicles
3099 GYKI 47261 dihydrochloride
Non-competitive AMPA antagonist
1454 GYKI 52466 dihydrochloride
Selective non-competitive AMPA antagonist
2555 GYKI 53655 hydrochloride
Non-competitive non-NMDA iGluR antagonist
4198 IEM 1925 dihydrobromide
Voltage- and use-dependent open-channel AMPA blocker
2766 Naspm trihydrochloride
Ca2+-permeable AMPA antagonist
0373 NBQX
Potent AMPA antagonist; more selective than CNQX (Cat. No. 0190)
1044 NBQX disodium salt
Potent AMPA antagonist; more water soluble form of NBQX (Cat. No. 0373)
2770 Philanthotoxin 74
GluA1 and GluA3 selective AMPA antagonist
0961 SYM 2206
Non-competitive AMPA antagonist
5032 Talampanel
Non-competitive non-NMDA iGluR antagonist
1765 UBP 282
Non-NMDA iGluR antagonist; distinguishes between motoneuron and dorsal root kainate receptors
2701 YM 90K hydrochloride
Selective AMPA antagonist
2345 ZK 200775
Competitive non-NMDA iGluR antagonist
Modulator
Cat. No. Product Name / Activity
4373 CMPDA
Positive allosteric modulator of GluA2 receptors
2980 CX 546
AMPA potentiator
5149 CX 614
Positive allosteric modulator of AMPA receptors
0713 Cyclothiazide
Positive allosteric modulator of AMPA receptors; inhibits AMPA desensitization
6278 JNJ 55511118
High affinity and selective negative modulator of AMPA receptors containing TARP-γ8
5297 LY 404187
Selective positive allosteric modulator of AMPA receptors
4900 PF 4778574
Positive allosteric modulator of AMPA receptors
3911 S 18986
Positive allosteric modulator of AMPA receptors
6353 UoS 12258
Positive allosteric modulator of AMPA receptors
Inhibitors
Cat. No. Product Name / Activity
867 Aniracetam
Inhibits desensitization; AMPA > kainate
1219 IDRA 21
Inhibits AMPA desensitization
1600 pep2-AVKI
Peptide inhibitor of GluA2 subunit binding to PICK1
1599 pep2-EVKI
Peptide inhibitor of GluA2 subunit binding to PICK1
1597 pep2-SVKI
Peptide inhibitor of GluA2 subunit binding to GRIP, ABP and PICK1; increases AMPA current amplitude
3801 Pep2m, myristoylated
Peptide inhibitor of GluA2 subunit binding to NSF; myristoylated form of pep2m (Cat. No. 1595).
Blockers
Cat. No. Product Name / Activity
1636 IEM 1460
Open-channel blocker of AMPA currents; selective for non-GluA2-containing receptors
4199 IEM 1754 dihydrobromide
Voltage-dependent, open-channel AMPA blocker
Others
Cat. No. Product Name / Activity
1048 1-BCP
Modulates AMPA-mediated responses
0964 Diazoxide
Inhibits AMPA desensitization
6094 2R,6R-Hydroxynorketamine hydrochloride
Ketamine metabolite; enhances AMPA currents; lacks ketamine-related side effects
6095 2S,6S-Hydroxynorketamine hydrochloride
Ketamine metabolite; decreases D-serine (a NMDA co-agonist); antidepressant
5982 cis-6-Hydroxynorketamine hydrochloride
Metabolite of ketamine (Cat.No. 3131); enhances AMPA currents
1602 Pep1-AGL
GluA1 subunit C-terminus peptide analog; also analog of Pep1-TGL (Cat. No. 1601)
1601 Pep1-TGL
GluA1 subunit C-terminus peptide analog
1598 pep2-SVKE
Inactive control peptide for pep2-SVKI (Cat. No. 1597)
1596 pep4c
Inactive control peptide for pep2m (Cat. No. 1595)
2973 Piracetam
Modulates Na+-flux at AMPA receptors; nootropic


Agonist
Cat. No. Product Name / Activity
1107 ATPA
Potent and selective GluK1 kainate agonist
0269 Domoic acid
Potent and selective kainate agonist
0307 (S)-(-)-5-Iodowillardiine
Highly potent and subtype-selective kainate agonist
0222 Kainic acid
Kainate agonist; excitant and neurotoxin
2225 MNI caged kainic acid
Caged kainic acid
0903 SYM 2081
Highly selective kainate agonist
Antagonist
Cat. No. Product Name / Activity
2728 ACET
Potent kainate antagonist; displays selectivity for GluK1-containing receptors
0190 CNQX
Potent and selective non-NMDA iGluR antagonist
1045 CNQX disodium salt
Potent non-NMDA iGluR antagonist; more water soluble form of Cat. No. 0190
0189 DNQX
Selective non-NMDA iGluR antagonist
2312 DNQX disodium salt
Selective non-NMDA iGluR antagonist; water-soluble salt of DNQX (Cat. No. 0189)
0845 Evans Blue tetrasodium salt
Non-NMDA iGluR antagonist; P2X antagonist; also inhibits L-glutamate uptake into synaptic vesicles
2555 GYKI 53655 hydrochloride
Non-competitive non-NMDA iGluR antagonist
2187 NS 3763
GluK1 selective and non-competitive kainate antagonist
5032 Talampanel
Non-competitive non-NMDA iGluR antagonist
3620 Topiramate
GluK1 antagonist; inhibits carbonic anhydrase (CA) II and IV; also positive allosteric modulator of GABAA receptors
1765 UBP 282
Non-NMDA iGluR antagonist; distinguishes between motoneuron and dorsal root kainate receptors
2078 UBP 296
Potent and selective kainate antagonist; selective for GluK1-containing receptors
1766 UBP 301
Kainate antagonist
2079 UBP 302
Potent and selective kainate antagonist; active enantiomer of UBP 296 (Cat. No. 2078)
3621 UBP 310
GluK1-selective kainate antagonist
2345 ZK 200775
Competitive non-NMDA iGluR antagonist
Ligand Sets
Cat. No. Product Name / Activity
1824 Kainate Receptor Tocriset™
Selection of 5 kainate receptor ligands (Cat. Nos. 0222110709031045 and 1454)
Others
Cat. No. Product Name / Activity
1777 Arctigenin
Binds to kainate receptors; neuroprotective. Also inhibits IκBα phosphorylation and MEK1
2207 PDZ1 Domain inhibitor peptide
Disrupts interaction between GluK2 and PSD-95 PDZ1 domain