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GABA and Glycine Receptor Modulators
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Description
Biochem/physiol Actions
Product #
21-Acetoxypregnenolone
A3750
ALX-1393 >98% (HPLC), powder
GlyT-2 glycine transporter inhibitor.
A5475
ALX 5407 hydrochloride >98% (HPLC), solid
Selective, irreversible GlyT-1 glycine transporter inhibitor.
A8977
(E)-4-Amino-2-butenoic acid solid
Potent GABA
c
receptor agonist.
T1694
γ-Aminobutyric acid ≥99%
Major inhibitory neurotransmitter in brain; GABA
A
and GABA
B
receptor agonist; increases Cl
−
conductance.
A2129
cis
-4-Aminocrotonic acid solid
GABA
C
receptor agonist
A201
3-Amino-1-propanesulfonic acid sodium salt ~98%
GABA
A
receptor agonist.
A4147
tert
-Butyl bicyclo[2.2.2]phosphorothionate solid
GABA
A
receptor antagonist; chloride channel blocker; extremely potent convulsant.
B104
Carbamazepine powder
Anticonvulsant; ligand for the GABA
A
receptor benzodiazepine modulatory site.
Sodium channel inhibitor
C4024
Carbamazepine meets USP testing specifications
Anticonvulsant; ligand for the GABA
A
receptor benzodiazepine modulatory site.
Sodium channel inhibitor
C8981
Chlormethiazole hydrochloride ≥98% (HPLC), crystalline
GABA
A
agonist; glycine receptor modulator.
C1240
Cloflubicyne ≥95% (NMR), solid
C1983
DEABL ≥98% (LC/MS), solid
Positive modulator of GABA
A
receptor; anticonvulsant
D1193
Dehydroisoandrosterone 3-sulfate sodium salt dihydrate ≥98%, powder
Dehydroisoandrosterone 3-sulfate sodium salt dihydrate is a negative allosteric modulator of GABA
A
receptors.
D5297
16-Dehydropregnenolone acetate ≥95%
D4875
3α,21-Dihydroxy-5α-
pregnan-20-one ≥95%
Positive allosteric modulator of GABA
A
receptors.
P2016
3α,12α-Dihydroxy-
5β-pregnan-20-one 3,12-diacetate
P5902
16,17-Epoxy-21-
acetoxypregnenolone ≥98%
E4625
16α,17α-
Epoxypregnenolone
E4875
16α,17α-
Epoxypregnenolone acetate ~95%
E5000
Etbicyphat ≥95% (NMR), solid
Blocker of neuronal voltage-dependent and GABA-gated chloride channels; non-competitive GABA antagonist; causes epileptiform seizures.
E5277
Etbicythionat ≥98% (NMR), solid
A potent non-competitive GABA antagonist in mammals; causes epileptiform seizures.
E5402
Etomidate >98% (HPLC), powder
Etomidate is a general anesthetic; potentiates GABAA transmission. The possible neuroprotective effect of etomidate against streptozotocin-induced (STZ-induced) hyperglycaemia were investigated in the rat brain and spinal cord. Etomidate treatment demonstrated neuroprotective effect on the neuronal tissue against the diabetic oxidative damage
E6530
Flucybene ≥95% (NMR), solid
A potent non-competitive GABA antagonist in mammals, molluscs and insects; convulsant.
F6551
Gabapentin solid
Anticonvulsant with unknown mechanism of action; crosses the blood brain barrier; increases GABA concentrations in the brain and reduces excitatory amino acid neurotransmission, perhaps through its effects on voltage-gated calcium channels; exhibits antinociceptive, anxiolytic, neuroprotective and anti-epileptic effects.
G154
Gaboxadol hydrochloride solid, ≥98% (HPLC)
GABA
A
receptor agonist.
T101
Ganaxolone solid
Ganaxolone (3alpha-hydroxy-3beta-methyl-5alpha-pregnane-20-one) is a positive allosteric modulator of the GABAA receptor subtype; synthetic analog of the endogenous neurosteroid allopregnanolone; effective against chemically induced seizures in rats and mice. Ganaxolone is an orally active analog of allopregnanolone that is not converted to the hormonally active 3-keto form. The enhanced anticonvulsant potency of ganaxolone after neurosteroid withdrawal supports the use of ganaxolone as a specific treatment for perimenstrual catamenial epilepsy.
G7795
Glycine
ReagentPlus
®
, ≥99% (TLC)
Inhibitory neurotransmitter in spinal cord, allosteric regulator of NMDA receptors.
G7126
Glycine hydrochloride ≥99% (TLC)
Inhibitory neurotransmitter in spinal cord, allosteric regulator of NMDA receptors.
G2879
Glycine sodium salt ≥99% (TLC)
Inhibitory neurotransmitter in spinal cord, allosteric regulator of NMDA receptors.
G6761
GS39783 ≥98% (HPLC), powder
Positive allosteric modulator of GABA
B
receptors
G5919
Guvacine hydrochloride ≥97% (NMR), solid
GABA uptake inhibitor.
G007
(1S,9R)-(+)-β-Hydrastine
Potent competitive GABA
A
receptor antagonist which is more potent than bicuculline; isolated from
Corydalis stricta
.
H8645
γ-Hydroxybutyric acid sodium salt
Endogenous GABA analog that induces absence-like seizures. It blocks dopamine release by blocking impulse flow in dopaminergic neurons.
H3635
17α-Hydroxypregnenolone
H5002
17α-Hydroxypregnenolone 3-acetate ≥98%
H5127
Hypotaurine ≥98% (TLC), powder
Antioxidant that binds hydroxyl radicals. Endogenous inhibitory neuromodulator that is blocked by strychnine and picrotoxin. Inhibits the Na
2+
-dependent transport of GABA and β-alanine. It is a degradation product of cysteine and a precursor of taurine.
H1384
Imidazole-4-acetic acid sodium salt
Competitive antagonist at GABA
C
receptors.
I7013
Isoguvacine hydrochloride solid
GABA
A
receptor agonist.
G002
16-Methylene-17α-
hydroxypregnenolone 3-acetate
M8626
Muscimol powder
GABA
A
receptor agonist.
M1523
Muscimol hydrobromide ≥98% (HPLC), solid
Muscimol hydrobromide is a GABA
A
receptor agonist.
G019
Nipecotic acid 98%
211672
NO-711 hydrochloride solid, ≥98% (HPLC)
Potent and selective GABA uptake inhibitor that crosses the blood-brain barrier.
N142
Phenylbenzene ω-phosphono-α-amino acid solid
Selective strychnine-sensitive glycine receptor antagonist.
P204
Picrotoxin powder
GABA
A
receptor antagonist; binds to the GABA receptor-linked Cl
−
channel.
P1675
Picrotoxinin
GABA
A
receptor antagonist; binds to the GABA receptor-linked Cl
−
channel.
P8390
Piperidine-4-sulfonic acid
GABA
A
receptor agonist.
P9159
5α-Pregnan-3α-ol-
11,20-dione powder, ≥98% (TLC)
Synthetic steroid compound alphaxalone (AFX) - 5α-Pregnan-3α-ol-11,20-dione- is a neurosteroid that directly activates and potentiates GABA
A
receptor-activated membrane current (IGABA). It acts as a positive allosteric modulator of the GABA
A
receptor; anesthetic. The alpha subunit subtype of GABA
A
determines the efficacy, but not the potency, of AFX neuroactive steroid to potentiate IGABA.
P5052
5α-Pregnan-3α-ol-
20-one solid
Positive allosteric modulator of GABA
A
chloride channel.
P8887
5α-Pregnan-3β-ol-
20-one 3β-acetate ≥98%
P8004
Pregnenolone sulfate sodium salt
Neurosteroid that antagonizes the GABA
A
receptor chloride channel.
P162
Propybicyphat 95% (NMR), solid
GABA-gated chloride channel blocker, non-competitive GABA antagonist in mammals.
P5489
Salicylidene salicylhydrazide ≥98% (HPLC), solid
Potent and selective inhibitor of α
2
β
1
γ
1
δ GABA
A
receptor subtype.
S8194
SB 205384 solid
GABA
A
receptor modulator selective for theα<ΣΥΒ>3β<SUB>2></SUB>γ
2</SUB>ΣΥΒS
subunit combination.
S7936
D
-Serine ≥98% (TLC)
Glycine mimic active at the strychnine-insensitive glycine binding site associated with the NMDA receptor as well as the inhibitory post-synaptic glycine receptor.
S4250
L
-Serine
ReagentPlus
®
, ≥99% (TLC)
Precursor of glycine by serine hydroxymethyltransferase.
S4500
SKF-89976A >98% (HPLC), solid
GABA transporter type 1 (GAT-1) inhibitor that crosses the blood brain barrier.
S9066
(
S
)-SNAP-5114 ≥98% (HPLC), solid
GABA transport inhibitor, showing selectivity for GAT-3 and GAT-2.
S1069
SR-95531 ≥98% (HPLC), solid
SR-95531 ia a specific GABA
A
receptor antagonist that does not affect GABA-transaminase or glutamate-decarboxylase activities.
S106
Strychnine
Convulsant; glycine receptor antagonist not associated with the NMDA receptor.
S0532
Strychnine hydrochloride
Convulsant; glycine receptor antagonist not associated with the NMDA receptor.
S8753
Taurine ≥99%
Non-selective endogenous agonist at glycine receptors. Conditionally essential sulfonated amino acid which modulates apoptosis in some cells; functions in many metabolic activities; a product of methionine and cysteine metabolism.
T0625
(1,2,5,6-Tetrahydropyridin-4-
yl)methylphosphinic acid hydrate ≥97% (HPLC), solid
TPMPA is a hybrid of isoguvacine and 3-APMPA designed to retain affinity for GABA
C
receptors but not to interact with GABA
A
or GABA
B
receptors. Electrical assays show that TPMPA is a competitive antagonist of cloned human mu 1 GABA
C
receptors expressed in
Xenopus laevis
oocytes (Kb approx. 2 μM). TPMPA is >100-fold weaker as an inhibitor of rat brain GABA
A
receptors expressed in oocytes (Kb approx. 320 μM) and has only weak agonist activity on GABA
B
receptors assayed in rat hippocampal slices (EC
50
approx. 500 μM). TPMP
A
may be used to investigate GABA
C
receptor function in the outer retina and in any other areas of the nervous system in which these types of receptor are present.
T200
(−)-α-Thujone purum, ≥96.0% (GC)
89231
Tofisopam ≥98% (HPLC), solid
Ligand for the GABA
A
receptor benzodiazepine modulatory site.
T8200
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