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GABA Metabolism and Transport

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PRODUCT NAMECATALOG #DESCRIPTIONCITATIONSRANKING
3-Methyl-GABAsc-2034713-Methyl-GABA is an activator of GABA aminotransferase. Anticonvulsant. CAS # 71424-95-8

2-Hydroxysaclofensc-2020112-Hydroxysaclofen is a sulphonic analogue of baclofen that acts as a selective GABAB antagonist. CAS # 117354-64-0

3α,12α-Dihydroxy-5β-pregnan-20-one 3,12-diacetatesc-226347 CAS # 15991-93-2

5-Nitro-α-oxo-N-(1R)-phenylethyl]-1H-indole-3-acetamidesc-358561TCS 1205 is reported to be a GABAA α1 partial agonist and GABAA α2 agonist in vitro. CAS # 355022-97-8

5α-Pregnan-3β-ol-20-one 3β-acetatesc-233497 CAS # 906-83-2

AA 29504sc-361096AA 29504 has been shown to be a positive allosteric modulator of GABAA receptors. CAS # 945828-50-2

β-Alaninesc-364682β-Alanine is an endogenous glycine agonist, more selective than Taurine (sc-202354). β-Alanine can also distinguish between GATs (GABA transporters). CAS # 107-95-9

DS2sc-294421DS2 is a positive allosteric modulator of δ-subunit containing GABAA receptors. CAS # 374084-31-8

16-Dehydropregnenolone acetatesc-224976 CAS # 979-02-2

Gabaculinesc-200473Gabaculine is a conformationally constrained analog of γ-aminobutyric acid (GABA). It acts as an irreversible and potent inhibitor of GABA transaminase. CAS # 59556-17-1

2
16,17-Epoxy-21-acetoxypregnenolonesc-224977 CAS # 28444-97-5

6,2'-Dihydroxyflavonesc-3000486,2'-Dihydroxyflavone is a partial inverse agonist at GABAA receptors with a-subunit selectivity.

16α,17α-Epoxypregnenolonesc-223173 CAS # 974-23-2

16α,17α-Epoxypregnenolone acetatesc-224978 CAS # 34209-81-9

17α-Hydroxypregnenolonesc-223186 CAS # 387-79-1

Flumazenil (Ro 15-1788)sc-200161Flumazenil is an antagonist to benzodiazepine binding on the GABAA receptor. CAS # 78755-81-4

10
17α-Hydroxypregnenolone 3-acetatesc-224980 CAS # 41906-06-3

MRK 016sc-358836MRK 016 is a selective GABAA receptor inverse agonist, displaying selectivity towards the the α5-subtype with an EC50= 3nM. CAS # 783331-24-8

Phenylbenzene ω-phosphono-α-amino acidsc-301540Phenylbenzene ω-phosphono-å-amino acid is a selective strychnine-sensitive glycine receptor (GlyR) antagonist.

21-Acetoxypregnenolonesc-231272 CAS # 566-78-9

17-PAsc-36107517-PA is a steroid analog that selectively antagonizes potentiation of GABA responses by 5α-reduced potentiating neurosteroids. CAS # 694438-95-4

(+/-)-β-Hydroxy-γ-butyrolactonesc-279196 CAS # 5469-16-9

SKF 89976A hydrochloridesc-203266SKF 89976A hydrochloride is a potent inhibitor of GABA uptake. Selectively inhibits the GABA T-1 transporter protein. CAS # 85375-85-5

CGP 7930sc-203543CGP 7930 is a positive allosteric modulator of GABAB receptors. CGP 7930 increases the potency and efficacy of GABA at both native and recombinant GABAB receptors CAS # 57717-80-3

Alphaxalonesc-203814Alphaxalone is a neurosteroid anesthetic that directly activates and potentiates GABAA receptor-activated membrane current (IGABA). CAS # 23930-19-0

β-CCBsc-204429β-CCB is a benzodiazepine inverse agonist, putative endogenous ligand. CAS # 84454-35-3

Dansyl-gamma-Amino-n-Butyric Acid Cyclohexylammonium Saltsc-294267 CAS # 76563-43-4

(±)-Baclofensc-200464A selective agonist of the GABAB metabotropic receptor. Produces muscle relaxant and antispastic effects. Prototypic agonist at GABAB. CAS # 1134-47-0

GABAsc-203053GABA is the major inhibitory neurotransmitter in the mammalian central nervous system. CAS # 56-12-2

1
(+)-Bicucullinesc-202498(+)-Bicuculline is an antagonist of the GABAA receptor. (+)-Bicuculline blocks the neurotransmission inhibition action of the GABA system. CAS # 485-49-4

Ganaxolonesc-203586Ganaxolone is a synthetic neurosteroid which functions as a stereoselective positive allosteric modulator of GABAA receptors. CAS # 38398-32-2

(-)-Bicuculline methiodidesc-200485(-)-Bicuculline methiodide is an N-methylated water-soluble derivative of the GABAA antagonist bicuculline. (-)-Bicuculline methiodide demonstrates blockade of Ca2+-activated K+ channel-mediated afterhyperpolarization. CAS # 40709-69-1

3
GS 39783sc-203589GS 39783 regulates GABAB receptors. CAS # 39069-52-8

(-)-Bicuculline methobromidesc-200436(-)-Bicuculline methobromide is an N-methylated water-soluble derivative of the GABAA antagonist bicuculline. CAS # 73604-30-5

(-)-Bicuculline methochloridesc-203528(-)-Bicuculline methochloride is a methochloride salt of (+)-bicuculline. This compound is a water-soluble GABAA antagonist. CAS # 53552-05-9

L-655,708sc-204040L-655,708 is a potent and selective inverse agonist for the benzodiazepine site of μ5-containing GABAA receptors. CAS # 130477-52-0

CGP 13501sc-203542CGP 13501 is a positive allosteric modulator at GABAB receptors, potentiating the effects of GABA at this receptor type. CAS # 56189-68-5

NCS-382 Sodium Saltsc-203444NCS-382 Sodium Salt is a γ -Hydroxybutyric acid antagonist, anticonvulsant. CAS # 131733-92-1

CGS 20625sc-203545CGS 20625 is an anti-anxiety drug used in research. CGS 20625 acts as a central benzodiazepine receptor partial agonist, but is classified as a nonbenzodiazepine drug. CAS # 111205-55-1

Pentylenetetrazolesc-203345Pentylenetetrazole causes alterations in excitatory and inhibitory neurotransmitter systems. CAS # 54-95-5

CGP 35348sc-361138CGP 35348 is a selective GABAB receptor antagonist (IC50= 34 μM). CGP 35348 has higher affinity for postsynaptic versus presynaptic receptors. CAS # 123690-79-9

CGP 36216sc-362724CGP 36216 is a selective GABAB antagonist. CGP 36216 also displays activity at presynaptic receptors and is found to be ineffective at GABAB postsynaptic receptors. CAS # 123691-29-2

CGP 46381sc-361140CGP 46381 is a selective GABAB receptor antagonist. CAS # 123691-14-5

trans-4-Hydroxycrotonic acidsc-203710trans-4-Hydroxycrotonic acid binds to the γ-hydroxybutyric acid (GHB) receptor with higher affinity than GHB itself. May be an endogenous ligand. CAS # 24587-49-3

CGP 52432sc-361141A selective and effective GABAB receptor antagonist CAS # 139667-74-6

CGP 54626 Hydrochloridesc-361142CGP 54626 Hydrochloride is a very potent and selective GABAb receptor antagonist. CAS # 149184-21-4

SKF-89976Asc-253567SKF 89976A is a GABA transporter type 1 inhibitor. This compound inhibits transport current competitively and transmitter-gated current non-competitively. CAS # 85375-15-1

Chlormethiazole hydrochloridesc-203548Chlormethiazole hydrochloride potentiates GABAA receptor function. Chlormethiazole hydrochloride is a sedative and anticonvulsant which is neuroprotective. CAS # 6001-74-7

Chlormezanonesc-203887Chlormezanone is a skeletal muscle relaxant, acting at the benzodiazapine site of GABAA receptors. CAS # 80-77-3

CI 966 hydrochloridesc-203891CI 966 hydrochloride is a selective inhibitor of GABA T-1 that is an anticonvulsive and neuroprotective displaying > 200-fold selectivity over GABA T-2 and GABA T-3. CAS # 110283-66-4

CL 218872sc-203552CL 218872 is a benzodiazepine agonist displaying selectivity for α1 subunit-containing GABAA receptors CAS # 66548-69-4

Cloflubicynesc-300382Cloflubicyne is a potent non-competitive GABA antagonist; convulsant; laboratory insecticide. CAS # 224790-70-9

DHEAsc-202573DHEA is a major secretory steroidal product of the adrenal gland. DHEA and its sulfated metabolite, DHEA-S, are negative modulators of GABAA receptors. CAS # 53-43-0

Dihydroergotoxine mesylatesc-203921Dihydroergotoxine mesylate binds with high affinity to GABAA receptor Cl- channel. Interacts with central dopaminergic, serotonergic and adrenergic (a1) receptors. Exhibits CAS # 8067-24-1

DMCM hydrochloridesc-205295DMCM hydrochloride is a benzodiazepine inverse agonist. Exhibits strong convulsant and anxiogenic activity. CAS # 82499-00-1

Etbicyphatsc-294479Etbicyphat is a synthetic, non-competitive GABA antagonist suggested to operate by blocking GABA-gated Cl- channels. CAS # 1005-93-2

Etomidatesc-203577Etomidate is a general anesthetic with GABA modulatory and GABA-mimetic actions. This compound is a GABAA receptors agonist. CAS # 33125-97-2

FG 7142sc-203952FG 7142 is an anxiogenic agent and benzodiazepine inverse agonist. FG 7142 shows increase in Tyr hydroxylation and exhibits upregulation of β-adrenoceptors in the cerebral cortex in mice. CAS # 78538-74-6

FGIN-1-43sc-203953FGIN-1-43 is a potent and specific ligand for mitochondrial diazepam binding inhibitor receptor. CAS # 145040-29-5

FrPbAIIsc-221630FrPbAII is a component of the Parawixia bistriata spider venom which has been shown to selectively inhibit GABA and glycine uptake (IC50=65 µM and 62 µM respectively) with little or no effect on monoamine or glutamate transporters.

gamma-Acetylenic GABAsc-295002Gamma-Acetylenic GABA is a GABA transaminase inhibitor. CAS # 57659-38-8

Nefiracetamsc-205766Nefiracetam is a nootropic of the racetam family. This compound activates L/N-type calcium channels, cholinergic, monoaminergic and GABAergic systems. CAS # 77191-36-7

GS 39783sc-300773GS 39783 is a positive allosteric modulator of GABAB receptors. CAS # 39069-52-8

Hispidulinsc-203999A natural flavanoid which acts as a potent benzodiazepine (BZD) receptor ligand. In addition, Hispidulin competitively binds to the benzodiazepine receptor, thus inhibiting 3H-Flumazenil from binding to the receptor. CAS # 1447-88-7

Indiplonsc-204011Potent GABAA receptor positive allosteric modulator. Exhibits sedative, hypnotic, anxiolytic and anticonvulsant activity in vivo and is orally active. CAS # 325715-02-4

Isoguvacine·HClsc-200451Isoguvacine HCl is an agonist of GABA (Gamma-amino butyric acid) receptors, the common inhibitory neurotransmitter of the central nervous system. CAS # 64603-90-3

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Loreclezole hydrochloridesc-204061Loreclezole hydrochloride is a subtype-selective GABAA receptor agonist. Positive allosteric modulator of β2 or β3-subunit containing receptors. CAS # 117857-45-1

Mebicyphatsc-295376Mebicyphat is shown to be a non-competitive GABA antagonist. Blocks GABA gated Cl- channels, and is shown to inhibit dihydropicrotoxin binding. CAS # 1449-89-4

Muscimolsc-200460Muscimol is a structural analog of GABA and a potent, selective agonist of the GABAA receptor. CAS # 2763-96-4

NCS-382 hydratesc-301458NCS-382 hydrate is a γ-Hydroxybutyrate (GHB) receptor antagonist. It displays anti-convulsant activity. CAS # 131733-92-1

(±)-Nipecotic acidsc-203645(±)-Nipecotic acid is a GABA uptake inhibitor (IC50 values are 8, 38, 106 and 2370 mM for hGABA T-1, rGABA T-2, hGABA T-3 and hBGT-1 respectively). CAS # 60252-41-7

NNC 05-2090 hydrochloridesc-204131NNC 05-2090 hydrochloride is a GABA uptake inhibitor; displays moderate selectivity for BGT-1 (mGAT-2) transporters. CAS # 184845-43-0

NNC 711sc-204132NNC 711 is a potent and selective inhibitor of GABA uptake by GABA T-1( (IC50 values are 0.04, 171, 1700 and 622 μM for hGABA T-1, rGABA T-2, hGABA T-3 and hBGT-1 respectively). CAS # 145645-62-1

Org 20599sc-204150Org 20599 is a positive allosteric modulator. Direct agonist of GABAA receptors at higher concentrations. CAS # 187652-71-7

Phaclofensc-200462Phaclofen is a selective GABAB receptor antagonist. The phosphonic acid derivative of Baclofen. CAS # 114012-12-3

Pregnenolone sulfate sodium saltsc-301609Pregnenolone sulfate sodium salt is a neurosteroid that has been demonstrated to antagonize the GABAA receptor chloride channel. CAS # 1852-38-6

Primidonesc-204861Primidone is an anticonvulsant. Potentiates GABAA receptor function. CAS # 125-33-7

Propybicyphatsc-301615Propybicyphat has demonstrated GABA-gated chloride channel blocker, and non-competitive GABA antagonist in mammals. CAS # 51486-74-9

R-(+)-Baclofen (free base)sc-203228R-(+)-Baclofen (free base) is a selective GABAB receptor agonist. By manipulating GABAB receptor activity using Baclofen, a variety of functions are studied including synaptic transmissions and antinociception events. CAS # 69308-37-8

R-(+)-Baclofen hydrochloridesc-203229A selective agonist of the GABAB receptor. 4.2-9.2-fold as effective as the S-(-) isomer. CAS # 63701-55-3

rac BHFFsc-204228Rac BHFF is a potent and selective GABAB receptor positive allosteric modulator that increases the efficacy and potency of GABA ( > 149% and > 15-fold respectively). Orally active and exhibits anxiolytic activity in vivo. CAS # 123557-91-5

Riluzolesc-201081Riluzole is a sodium channel protein inhibitor and potent neuroprotective agent. CAS # 1744-22-5

RO 15-4513sc-203683A high affinity benzodiazepine ligand which acts as a partial inverse agonist at recombinant diazepam-sensitive (DS) benzodiazepine α1-, α2-, α3- and α5-GABAA receptors. CAS # 91917-65-6

RO 19-4603sc-203684RO 19-4603 is a benzodiazepine inverse agonist and binds with high affinity to both diazepam-sensitive (DS) and diazepam-insensitive (DI) GABAA receptors (Ki values are ~ 0.2 and ~ 2.6 nM for DS and DI receptors respectively). CAS # 99632-94-7

S(+)-gamma-Vinyl-GABAsc-222279S(+)-gamma-Vinyl-GABA is a selective GABA transaminase inhibitor and active enantiomer. S(+)-gamma-Vinyl-GABA may be potentially useful in treating cocaine addiction. CAS # 74046-07-4

(S)-SNAP 5114sc-204257(S)-SNAP 5114 is a GABA uptake inhibitor, showing selectivity for GABA T-3 and GABA T-2 (IC50 values are 5, 21 and 388 µM for hGABA T-3, rGABA T-2 and hGABA T-1 respectively). CAS # 157604-55-2

Saclofensc-203252Saclofen is a selective antagonist of the GABAB receptor. CAS # 125464-42-8

SB 205384sc-204263SB 205384 is a GABAA receptor modulator; slows current decay. Displays some specificity for α3-subunit-containing receptors (in particular α3β2γ2). CAS # 160296-13-9

SCSsc-203375SCS is a potent and selective partial inhibitor of β1-containing GABAA receptors. SCS may bind allosterically to a novel site on GABAA receptor. CAS # 3232-36-8

SK&F 97541sc-200469SK&F 97541 is a very potent GABAB agonist, at least ten times more active than baclofen. CAS # 127729-35-5

SR 95531 Hydrobromidesc-203701SR 95531 Hydrobromide is a selective GABAA receptor antagonist. This compound displaces [3H]-GABA with a Ki of 150 nM. CAS # 104104-50-9

TACAsc-203705TACA is a GABAA and GABAC agonist. TACA is also a GABA-T substrate and GABA uptake inhibitor. This compound is a trans-isomer of CACA. CAS # 38090-53-8

TB 21007sc-204322TB 21007 is a GABAA receptor inverse agonist selective for the α5-subtype (Ki values are 1.6, 16, 20 and 20 nM for α5, α2, α1 and α3 subtypes respectively). CAS # 207306-50-1

Thiocolchicosidesc-202839Thiocolchicoside is a potent, competitive antagonist of GABAA receptors. CAS # 602-41-5

Thiomuscimolsc-213035Thiomuscimol is a structural analog used as a photoaffinity label for GABAA. Thiomuscimol also inhibits [3H]muscimol binding to brain GABAA receptors. CAS # 62020-54-6

THIP hydrochloridesc-204342THIP hydrochloride is a systemically active GABAA receptor agonist and GABAC receptor antagonist. CAS # 64603-91-4

TPMPAsc-204352TPMPA is a competitive, selective GABAC antagonist with minimal effects on GABAA and GABAB receptors. CAS # 182485-36-5

Tracazolate hydrochloridesc-203709Tracazolate hydrochloride is a subtype selective GABAA allosteric receptor modulator. CAS # 41094-88-6

U 89843Asc-204361U 89843A is a positive allosteric modulator of GABAA receptors. Enhances GABA-induced Cl- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. CAS # 157013-32-6

U 90042sc-204362U 90042 is a GABAA receptor ligand that binds with comparable affinities to three receptor subtypes: α1β2γ2, α3β2γ2 and α6β2γ2 (Ki values are 7.8, 9.5 and 11.0 nM respectively). CAS # 134516-99-7

U 93631sc-204364U 93631 is a GABAA receptor antagonist that binds picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. CAS # 152273-12-6

Valerenic acidsc-204377Valerenic acid is a positive allosteric modulator of GABAA receptors that displays preference for β2 or β3 subunit receptors. CAS # 3569-10-6

1
Vigabatrinsc-204382Vigabatrin is a selective GABA transaminase (T) inhibitor. CAS # 60643-86-9

ZAPA sulfatesc-200471ZAPA sulfate is a potent, selective GABAA receptor agonist. Demonstrates higher GABAA affinity than muscimol and GABA. CAS # 92138-10-8

ZK 93423 hydrochloridesc-204422ZK 93423 hydrochloride is a potent benzodiazepine agonist. Non-selective with GABAA receptors containing α1-, α2-, α3- and α5-subunits. CAS # 83910-44-5

ZK 93426 hydrochloridesc-203727ZK 93426 hydrochloride is a potent, selective and competitive benzodiazepine receptor antagonist. CAS # 89592-45-0

Guvacine hydrochloridesc-263347Guvacine hydrochloride inhibits GABA uptake (IC50 values are 14, 58, 119 and 1870 μM for hGABA T-1, rGABA T-2, hGABA T-3 and hBGT-1 respectively). CAS # 6027-91-4

Tiagabine Hydrochloridesc-208437Tiagabine Hydrochloride is an uptake inhibitor ( (IC50 = 67 nM in vivo)) of GABA and also an anticonvulsant. Tiagabine Hydrochloride shows a high affinity for GABA T-1. CAS # 145821-59-6