Antagonists

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89231 (−)-α-Thujone ≥96.0% (GC) GABAA receptor antagonist.
T200 (1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid hydrate ≥97% (NMR), solid TPMPA is a hybrid of isoguvacine and 3-APMPA designed to retain affinity for GABAC receptors but not to interact with GABAA or GABAB receptors. Electrical assays show that TPMPA is a competitive antagonist of cloned human mu 1 GABAC receptors expressed in Xenopus laevis oocytes (Kb approx. 2 μM). TPMPA is >100-fold weaker as an inhibitor of rat brain GABAA receptors expressed in oocytes (Kb approx. 320 μM) and has only weak agonist activity on GABAB receptors assayed in rat hippocampal slices (EC50 approx. 500 μM). TPMPA may be used to investigate GABAC receptor function in the outer retina and in any other areas of the nervous system in which these types of receptor are present.
B7561 1(S),9(R)-(−)-Bicuculline methbromide ≥98% (HPLC), solid 1(S),9(R)-(−)-Bicuculline methbromide is a GABAA receptor antagonist, which blocks Ca2+-activated potassium (SK) channels. It is the water-soluble derivative of (+)-bicuculline.
B7686 1(S),9(R)-(−)-Bicuculline methchloride ≥97% (HPLC), powder 1(S),9(R)-(−)-Bicuculline methchloride is a GABAA receptor antagonist, which blocks Ca2+-activated potassium (SK) channels.
SML0706   2-AEMP trifluoroacetate salt ≥97% (NMR) 2-AEMP is a competitive GABAC antagonist with a rapid onset of, and release from inhibition.
A6566 2-Hydroxysaclofen ≥98% (TLC), solid Potent and selective antagonist at GABAB receptors.
C5851 CGP 35348 hydrate ≥97% (NMR), solid CGP 35348 hydrate is a GABAB-receptor antagonist.
SML0594   CGP 55845 hydrochloride ≥98% (HPLC) CGP 55845 is a potent selective GABA-B receptor antagonist with an IC50 of 5 nM.
SML0475 CGP36742 ≥97% (NMR) CGP36742 was the first orally active GABAB-selective antagonist. The IC50 for blocking GABAergic transmission is 36 μM. Oral administration of CGP36742 in rats blocks baclofen-induced neuronal depression, and reduces learning deficit and passive avoidance in an olfactory bulbectomy depression model.
SML0593   CGP52432 ≥98% (HPLC) CGP52432 is a very potent antagonist of GABAB receptors. (IC50 = 85 nM).
SML0645   Iomazenil ≥98% (HPLC) Iomazenil (Ro 16–0154) is a benzodiazepine competitive antagonist and partial inverse agonist. Iomazenil has been shown to counteract the effects of alcohol.
P118 Phaclofen solid Phaclofen plays a vital role in identifying the physiological importance of central and peripheral bicuculline-insensitive receptors with which GABA and (−) baclofen interact. Phaclofen acts as a GABAB receptor antagonist. Phaclofen has an ability to reversibly block the late, bicuculline resistant, K+ dependent inhibitory postsynaptic potential (IPSP) logged in projection cells of the cat and rat dorsal lateral geniculate nucleus and in rat hippocampal CA1 pyramidal neurons.
P8390 Picrotoxinin GABAA receptor antagonist; binds to the GABA receptor-linked Cl channel.
P1675 Picrotoxin powder GABAA receptor antagonist; binds to the GABA receptor-linked Cl channel.
P5489 Propybicyphat 95% (NMR), solid GABA-gated chloride channel blocker, non-competitive GABA antagonist in mammals.
S9066 SKF-89976A >98% (HPLC), solid GABA transporter type 1 (GAT-1) inhibitor that crosses the blood brain barrier.
SKF-89976A contains a cyclic amino acid with lipophilic moiety that enables the compound to cross the blood-brain barrier.1,2 It decreases the excitotoxic swelling of chick retina cells by blocking the glutamate-induced GABA release.3
S106 SR-95531 ≥98% (HPLC), powder SR-95531 is a specific GABAA receptor antagonist that does not affect GABA-transaminase or glutamate-decarboxylase activities.
S166 Saclofen solid Saclofen is the sulphonic analog of baclofen and is a selective GABAB receptor antagonist.
B104 tert-Butyl bicyclo[2.2.2]phosphorothionate solid GABAA receptor antagonist; chloride channel blocker; extremely potent convulsant.