GABA analogue

Short description: Class of drugs

γ-Aminobutyric acid (GABA)

A GABA analogue is a compound which is an analogue or derivative of the neurotransmitter gamma-Aminobutyric acid (GABA) (the IUPAC of which is 4-aminobutanoic acid).

Many GABA analogues are used as drugs, especially as anticonvulsants, sedatives, and anxiolytics.

## Contents

* 1 List of GABA analogues
* 1.1 Deaminated
* 1.1.1 3- or 4-Hydroxylated
* 1.2 β-Substituted
* 1.3 Cyclized
* 1.4 GABA prodrugs
* 1.5 Others/miscellaneous
* 2 See also
* 3 References

## List of GABA analogues

### Deaminated

* Butyric acid (butanoic acid) – histone deacetylase inhibitor and full agonist of free fatty acid receptor 2, free fatty acid receptor 3, and niacin receptor 1
* Derivatives: butyrate (butanoate), sodium butyrate, methyl butyrate, ethyl butyrate, butyl butyrate, pentyl butyrate
* Valeric acid (pentanoic acid) – constituent of valerian; has an unpleasant odor and fruity flavor and esters are used as additives
* Derivatives: valerate (pentanoate), methyl valerate, ethyl valerate, pentyl valerate
* Isovaleric acid (isopentanoic acid/3-methylbutanoic acid) – constituent of valerian; has anticonvulsant effects; PAM of the GABAA receptor
* Derivatives: isovalerate (isopentanoate/3-methylbutanoate), menthyl isovalerate (validolum) – used as an anxiolytic and sedative in Russia
* Isovaleramide (isopentamide/3-methylbutanamide) – constituent of valerian; has anxiolytic and sedative effects; PAM of the GABAA receptor
* Valproic acid (2-propylpentanoic acid) – anticonvulsant/mood stabilizer; inhibitor of HDAC, SSADH, and GABA-T, blocker of VDSCs and GABA reuptake, AR/PR antagonist
* Derivatives: sodium valproate, valproate semisodium, divalproex sodium, valproate pivoxil
* Valpromide (2-propylpentanamide) – anticonvulsant; same mechanism of action as valproic acid, plus inhibitor of epoxide hydrolase
* Valnoctamide (2-ethyl-3-methylpentanamide) – anticonvulsant; similar mechanism of action to valproic acid; structural isomer of valpromide

#### 3- or 4-Hydroxylated

* 3-Hydroxybutanal – synthetic hypnotic and sedative drug
* GHB (γ-hydroxybutyric acid) – neurotransmitter, drug of abuse; agonist of GHB receptor and GABAB receptor
* Derivatives: sodium oxybate (sodium γ-hydroxybutanoate) – used to treat narcolepsy; same mechanism of action as GHB
* Aceburic acid (γ-hydroxybutyric acid acetate) – synthetic prodrug to GHB
* GBL (γ-hydroxybutyric acid lactone) – metabolic intermediate and prodrug to GHB
* GHBAL (γ-hydroxybutyraldehyde or γ-hydroxybutanal) – metabolic intermediate and prodrug to GHB
* GHV (γ-hydroxyvaleric acid) – designer drug; analogue of GHB with similar effects
* GVL (γ-valerolactone) – designer drug; prodrug to GHV
* T-HCA/GHC (γ-hydroxycrotonic acid) – neurotransmitter; GHB receptor agonist
* GCL (γ-crotonolactone) – prodrug to T-HCA/GHC
* HOCPCA (3-hydroxycyclopent-1-enecarboxylic acid) – synthetic GHB receptor agonist
* UMB68 (γ-hydroxy-γ-methylpentanoic acid) – synthetic GHB receptor agonist

### β-Substituted

* GABOB (β-hydroxy-GABA) – anticonvulsant; GABA receptor agonist
* Pregabalin (β-isobutyl-GABA) – analgesic, anticonvulsant, and anxiolytic; potent inhibitor of α2δ subunit-containing VGCCs.
* Phenibut (β-phenyl-GABA) – sedative and anxiolytic from Russia; GABAB receptor agonist, and to a lesser extent inhibitor of α2δ subunit-containing VGCCs.
* Baclofen (β-(4-chlorophenyl)-GABA) – antispasmodic drug; potent GABAB receptor agonist, weak inhibitor of α2δ subunit-containing VGCCs
* Tolibut (β-(4-methylphenyl)-GABA) – analgesic, tranquilizing, and neuroprotective drug
* Phaclofen (phosphonobaclofen) – GABAB receptor antagonist
* Saclofen (sulfonobaclofen) – GABAB receptor antagonist

### Cyclized

* Arecaidine – constituent of areca nuts; GABA reuptake inhibitor
* Gabaculine – neurotoxin; GABA-T inhibitor and GABA reuptake inhibitor
* Gabapentin – anticonvulsant; inhibitor of α2δ subunit-containing VGCCs
* Gabapentin enacarbil – used for the treatment of restless legs syndrome and postherpetic neuralgia; same mechanism of action as gabapentin
* Gaboxadol – GABAA receptor agonist
* Guvacine – constituent of areca nuts; GABA reuptake inhibitor
* Isoguvacine – GABAA receptor agonist
* Isonipecotic acid – GABAA receptor partial agonist
* Muscimol – constituent of Amanita muscaria mushrooms; GABAA receptor agonist
* Nipecotic acid – used in scientific research; GABA reuptake inhibitor

### GABA prodrugs

* Cetyl-GABA – anticonvulsant
* L-Glutamine – endogenous precursor of GABA and glutamate
* N-Benzoyl-GABA – not confirmed to be a GABA prodrug
* N-Isonicotinoyl-GABA – structural isomer of picamilon – not confirmed to be a GABA prodrug
* Picamilon (N-nicotinoyl-GABA) – dietary supplement and prescription drug in Russia – not confirmed to be a GABA prodrug
* Pivagabine (N-pivaloyl-GABA) – turned out not to be a prodrug of GABA
* Progabide (complex structure) – anticonvulsant
* Tolgabide (complex structure) – anticonvulsant

### Others/miscellaneous

* 1,4-Butanediol – metabolic intermediate and prodrug to GHB
* 3-Methyl-GABA – GABA-T activator
* AABA/homoalanine (α-aminobutyric acid) – used by nonribosomal peptide synthetases
* BABA (β-aminobutyric acid) – known for its ability to induce plant disease resistance
* DAVA (δ-aminopentanoic acid) – GABA receptor agonist
* Gabamide (γ-aminobutanamide) – GABA receptor agonist
* Gabazine (SR-95531) – antagonist of the GABAA and GHB receptors
* GAVA (γ-aminopentanoic acid) – GABA reuptake inhibitor
* Glufimet (dimethyl 3-phenylglutamate hydrochloride) – experimental drug related to phenibut
* Glutamic acid (glutamate) – neurotransmitter
* Homotaurine (tramiprosate) – GABAA receptor agonist, GABAB receptor antagonist
* Hopantenic acid (N-pantoyl-GABA) – central nervous system depressant used in Russia
* Isovaline – peripherally selective agonist of the GABAB receptor
* Lesogaberan (AZD-3355) – agonist of the GABAB receptor
* N-Anisoyl-GABA – major active metabolite of the nootropic aniracetam
* NCS-382 – antagonist of the GHB receptor
* Piracetam and other racetams[1] – nootropics
* Pivagabine (N-pivaloyl-GABA) – antidepressant/anxiolytic drug; CRF inhibitor
* Vigabatrin (y-vinyl-GABA) – anticonvulsant; GABA-T inhibitor

## See also

* Bamaluzole
* Bicuculline
* Deramciclane
* Ethanol
* Fengabine
* Gabapentinoid
* Loreclezole
* Propofol
* Retigabine/ezogabine
* Tiagabine
* Valerenic acid

## References

1. ↑ John Scott Werry; Michael G. Aman (29 June 2013). Practitioner's Guide to Psychoactive Drugs for Children and Adolescents. Springer Science & Business Media. pp. 415–. ISBN 978-1-4899-0086-9. https://books.google.com/books?id=k_2fBwAAQBAJ&pg=PA415.

{{Navbox | name = GABA receptor modulators | title = GABA receptor modulators | state = collapsed | bodyclass = hlist | groupstyle = text-align:center;

| group1 = Ionotropic
|  list1 = {{Navbox|subgroup
| groupstyle = text-align:center
| groupwidth = 5em

| group1 = GABAA
| list1  =

* Agonists: (+)-Catechin
* Bamaluzole
* Barbiturates (e.g., phenobarbital)
* BL-1020
* DAVA
* Dihydromuscimol
* GABA
* Gabamide
* GABOB
* Gaboxadol (THIP)
* Homotaurine (tramiprosate, 3-APS)
* Ibotenic acid
* iso-THAZ
* iso-THIP
* Isoguvacine
* Isomuscimol
* Isonipecotic acid
* Kojic amine
* Lignans (e.g., honokiol)
* Methylglyoxal
* Monastrol
* Muscimol
* Nefiracetam
* Neuroactive steroids (e.g., allopregnanolone)
* Org 20599
* PF-6372865
* Phenibut
* Picamilon
* P4S
* Progabide
* Propofol
* Quisqualamine
* SL-75102
* TACA
* TAMP
* Terpenoids (e.g., borneol)
* Thiomuscimol
* Tolgabide
* ZAPA

* Positive modulators (abridged; see here for a full list): α-EMTBL
* Alcohols (e.g., ethanol)
* Anabolic steroids
* Avermectins (e.g., ivermectin)
* Barbiturates (e.g., phenobarbital)
* Benzodiazepines (e.g., diazepam)
* Bromide compounds (e.g., potassium bromide)
* Carbamates (e.g., meprobamate)
* Carbamazepine
* Chloralose
* Chlormezanone
* Clomethiazole
* Dihydroergolines (e.g., ergoloid (dihydroergotoxine))
* Etazepine
* Etifoxine
* Fenamates (e.g., mefenamic acid)
* Flavonoids (e.g., apigenin, hispidulin)
* Fluoxetine
* Flupirtine
* Imidazoles (e.g., etomidate)
* Kava constituents (e.g., kavain)<!--PMID: 9776662-->
* Lanthanum
* Loreclezole
* Monastrol
* Neuroactive steroids (e.g., allopregnanolone, [[Chemistry:Cholecholesterol]], THDOC)
* Niacin
* Nicotinamide (niacinamide)
* Nonbenzodiazepines (e.g., β-carbolines (e.g., [[abecarnil), cyclopyrrolones (e.g., zopiclone), imidazopyridines (e.g., zolpidem), pyrazolopyrimidines (e.g., zaleplon))
* Norfluoxetine
* Petrichloral
* Phenols (e.g., propofol)
* Phenytoin
* Piperidinediones (e.g., glutethimide)
* Propanidid
* Pyrazolopyridines (e.g., etazolate)
* Quinazolinones (e.g., methaqualone)
* Retigabine (ezogabine)
* ROD-188
* Skullcap constituents (e.g., baicalin)
* Stiripentol
* Sulfonylalkanes (e.g., sulfonmethane (sulfonal))
* Topiramate
* Valerian constituents (e.g., valerenic acid)
* Volatiles/gases (e.g., chloral hydrate, chloroform, [[Chemistry:Diethyl diethyl ether, Parparaldehyde]], sevoflurane)

* Antagonists: Bicuculline
* Coriamyrtin
* Dihydrosecurinine
* Gabazine (SR-95531)
* Hydrastine
* Hyenachin (mellitoxin)
* PHP-501
* Pitrazepin
* Securinine
* Sinomenine
* SR-42641
* SR-95103
* Thiocolchicoside
* Tutin

* Negative modulators: 1,3M1B
* 3M2B
* 11-Ketoprogesterone
* 17-Phenylandrostenol
* α5IA (LS-193,268)
* β-CCB
* β-CCE
* β-CCM
* β-CCP
* β-EMGBL
* Anabolic steroids
* Amiloride
* Anisatin
* β-Lactams (e.g., penicillins, cephalosporins, carbapenems)
* Basmisanil
* Bemegride
* Bicyclic phosphates (TBPS, TBPO, IPTBO)
* BIDN
* Bilobalide
* Bupropion
* CHEB
* Chlorophenylsilatrane
* Cicutoxin
* Cloflubicyne
* Cyclothiazide
* DHEA
* DHEA-S
* Dieldrin
* (+)-DMBB
* DMCM
* DMPC
* EBOB
* Etbicyphat
* FG-7142 (ZK-31906)
* Fiproles (e.g., fipronil)
* Flavonoids (e.g., amentoflavone, oroxylin A)
* Flumazenil
* Fluoroquinolones (e.g., ciprofloxacin)
* Flurothyl
* Furosemide
* Golexanolone
* Iomazenil (123I)
* IPTBO
* Isopregnanolone (sepranolone)
* L-655,708
* Laudanosine
* Leptazol
* Lindane
* MaxiPost
* Morphine
* Morphine-3-glucuronide
* MRK-016
* Naloxone
* Naltrexone
* Nicardipine
* Nonsteroidal antiandrogens (e.g., [[apalutamide, [[Chemistry:Bicalutbicalutamide, Enzalutenzalutamide, Chemistry:Flutamide|flut]]amide]], nilutamide)
* Oenanthotoxin
* Pentylenetetrazol (pentetrazol)
* Phenylsilatrane
* Picrotoxin (i.e., picrotin, picrotoxinin and dihydropicrotoxinin)
* Pregnenolone sulfate
* Propybicyphat
* PWZ-029
* Radequinil
* Ro 15-4513
* Ro 19-4603
* RO4882224
* RO4938581
* Sarmazenil
* SCS
* Suritozole
* TB-21007
* TBOB
* TBPS
* TCS-1105
* Terbequinil
* TETS
* Thujone
* U-93631
* Zinc
* ZK-93426

| group2 = GABAA-ρ
| list2  =

* Agonists: BL-1020
* CACA
* CAMP
* Homohypotaurine
* GABA
* GABOB
* Ibotenic acid
* Isoguvacine
* Muscimol
* N4-Chloroacetylcytosine arabinoside
* Picamilon
* Progabide
* TACA
* TAMP
* Thiomuscimol
* Tolgabide

* Positive modulators: Allopregnanolone
* Alphaxolone
* ATHDOC
* Lanthanides

* Antagonists: (S)-2-MeGABA
* (S)-4-ACPBPA
* (S)-4-ACPCA
* 2-MeTACA
* 3-APMPA
* 4-ACPAM
* 4-GBA
* cis-3-ACPBPA
* CGP-36742 (SGS-742)
* DAVA
* Gabazine (SR-95531)
* Gaboxadol (THIP)
* I4AA
* Isonipecotic acid
* Loreclezole
* P4MPA
* P4S
* SKF-97541
* SR-95318
* SR-95813
* TPMPA
* trans-3-ACPBPA
* ZAPA

* Negative modulators: 5α-Dihydroprogesterone
* Bilobalide
* Loreclezole
* Picrotoxin (picrotin, picrotoxinin)
* Pregnanolone
* ROD-188
* THDOC
* Zinc

| group2 = Metabotropic

| list2 =

GABAB|

* Agonists: 1,4-Butanediol
* 4-Fluorophenibut
* Aceburic acid
* Arbaclofen
* Arbaclofen placarbil
* Baclofen
* BL-1020
* GABA
* Gabamide
* GABOB
* GBL
* GHB
* GHBAL
* GHV
* GVL
* Isovaline
* Lesogaberan
* Phenibut
* Picamilon
* Progabide
* Sodium oxybate
* SKF-97,541
* SL 75102
* Tolgabide
* Tolibut

* Positive modulators: ADX-71441
* BHF-177
* BHFF
* BSPP
* CGP-7930
* CGP-13501
* GS-39783
* rac-BHFF
* KK-92A

* Antagonists: 2-Hydroxysaclofen
* CGP-35348
* CGP-46381
* CGP-52432
* CGP-54626
* CGP-55845
* CGP-64213
* DAVA
* Homotaurine (tramiprosate, 3-APS)
* Phaclofen
* Saclofen
* SCH-50911
* SKF-97541

* Negative modulators: Compound 14

|

| below =

See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators

* v
* t
* e

GHB receptor modulators

Receptor
(ligands)|

| GHBR|

* Agonists: Main site: 1,4-BD
* 3-HPA
* Aceburic acid (GHB acetate)
* BDDA (DABD)
* EAB
* GBL
* GCL
* GHB
* GHBAL
* GHV (4-methyl-GHB)
* GVL
* HOCHCA
* HOCPCA
* MAB
* NCS-356
* NCS-435
* Sodium oxybate
* T-HCA (GHC)
* THF
* UMB58
* UMB66
* UMB68
* UMB72
* UMB73
* UMB86; Positive allosteric modulators: (+)-Catechin
* Monastrol

* Antagonists: Main site: Gabazine (SR-95531)
* NCS-382

* Unknown/unsorted: Main site: 2-HPA
* 3-Methyl-GHB
* 3-Methyl-THCA
* 4-Benzyl-GHB
* 4-HPBA
* 4-Methyl-THCA
* 4-Phenyl-GHB
* 4-Phenyl-THCA
* Amisulpride
* azido-BnOPh-GHB
* BnOPh-GHB
* DHV
* DVL
* GTBL
* Levosulpiride
* NCS-400
* Prochlorperazine
* Sulpiride
* Sultopride
* UMB108
* UMB109
* UMB119

|

GABAB|

* See here instead.

Transporter
(blockers)|

| MCTs|

* α-Ketoisocaproate
* Acetoacetic acid
* AR-C155858
* Atorvastatin
* Benzoic acid
* BHB
* Butyric acid
* CHCA
* DBDS
* DIDS
* Hexanoic acid
* Lactic acid
* Luteolin
* Niflumic acid
* NPPB
* Phenylpyruvic acid
* Phloretin
* Probenecid
* Pyruvic acid
* Quercetin
* Salicylic acid
* Simvastatin
* Sodium valproate
* Valproic acid

|

SMCTs|

* Benzoic acid
* BHB
* Butyric acid
* Fenoprofen
* Ibuprofen
* Ketoprofen
* Mesalazine (5-ASA)
* Naproxen
* Nicotinic acid
* Probenecid
* Propionic acid
* Pyruvic acid
* Salicyclic acid

VIATT|

* β-Alanine
* Bafilomycin A1
* Butyric acid
* Chicago Sky Blue 6B
* Evans Blue
* GABA
* Glycine
* Nigericin
* Nipecotic acid
* Valinomycin
* Vigabatrin

Enzyme
(inhibitors)|

| SSR|

* Quercetin

|

GHBDH|

* α-Ketoisocaproic acid
* Ethosuximide
* Phenylacetate
* Salicylic acid
* Valproic acid

* Enhancers: D-Glucuronic acid

HOT|

* Cyanide
* Phenanthroline

ADH|

* Cimetidine
* Ethanol
* Fomepizole (4-methylpyrazole)
* Pyrazole

ALDH|

* Acetaldehyde
* Cimetidine
* Cyanamide
* Disulfiram
* Prunetin

See also
Receptor/signaling modulators
GABA receptor modulators
Glutamate receptor modulators
Glycine receptor modulators

* v
* t
* e

Ion channel modulators

Calcium|

| VDCCs|

| Blockers|

* L-type-selective: Dihydropyridines: Amlodipine
* Aranidipine
* Azelnidipine
* Barnidipine
* Clevidipine
* Cronidipine
* Darodipine
* Dexniguldipine
* Elgodipine
* Elnadipine
* Felodipine
* Flordipine
* Furnidipine
* Iganidipine
* Isradipine
* Lacidipine
* Lemildipine
* Lercanidipine
* Levamlodipine
* Levniguldipine
* Manidipine
* Mepirodipine
* Mesudipine
* Nicardipine
* Nifedipine
* Niguldipine
* Niludipine
* Nilvadipine
* Nimodipine
* Nisoldipine
* Nitrendipine
* Olradipine
* Oxodipine
* Palonidipine
* Pranidipine
* Ryodipine (riodipine)
* Sagandipine
* Sornidipine
* Teludipine
* Tiamdipine
* Trombodipine
* Vatanidipine; Diltiazem derivatives: Clentiazem
* Diltiazem
* Iprotiazem
* Nictiazem
* Siratiazem; Phenylalkylamines: Anipamil
* Dagapamil
* Devapamil
* Dexverapamil
* Emopamil
* Etripamil
* Falipamil
* Gallopamil
* Levemopamil
* Nexopamil
* Norverapamil
* Ronipamil
* Tiapamil
* Verapamil; Others: AH-1058
* Brinazarone
* Budiodarone
* Celivarone
* Cyproheptadine
* Dronedarone
* Fantofarone
* SR-33805
* Tetrahydropalmatine

* N-type-selective: ω-Conotoxins
* ω-Conotoxin GVIA
* Caroverine
* Huwentoxin XVI
* Leconotide (ω-conotoxin CVID)
* PD-173212
* Ralfinamide
* Safinamide
* Z160
* Ziconotide (ω-conotoxin MVIIA)

* P-type-selective: ω-Agatoxin IVA
* ω-Agatoxin IVB

* R-type-selective: SNX-482

* T-type-selective: ABT-639
* ML-218
* Niflumic acid
* NNC 55-0396
* ProTx I
* Z944
* Zonisamide

* Non-selective: ω-Agatoxin TK
* ω-Conotoxin MVIIC
* Benidipine
* Bepridil
* Cilnidipine
* Cinnarizine
* Dotarizine
* Efonidipine
* Flunarizine
* Lamotrigine
* Levetiracetam
* Lomerizine
* Loperamide
* Mibefradil
* NP078585
* Ruthenium red
* TROX-1

* α2δ subunit-selective (gabapentinoids): 4-Methylpregabalin
* Arbaclofen
* Arbaclofen placarbil
* Atagabalin
* Baclofen
* Gabapentin
* Gabapentin enacarbil
* Imagabalin
* Mirogabalin
* PD-200,347
* PD-217,014
* PD-299,685
* Phenibut
* Pregabalin

* Others/unsorted: Bencyclane
* Berbamine
* Bevantolol
* Canadine
* Carboxyamidotriazole
* Cycleanine
* Dauricine
* Dimeditiapramine
* Diproteverine
* Enpiperate
* Eperisone
* Elpetrigine
* Ethadione
* Ethanol (alcohol)
* Ethosuximide
* Fasudil
* Fendiline
* Fostedil
* Imepitoin
* JTV-519
* Lidoflazine
* Magnesium
* Manoalide
* Mesuximide
* Monatepil
* Naftopidil
* Ochratoxin A
* Osthol
* Otilonium bromide
* Paramethadione
* Phensuximide
* Pinaverium bromide
* Prenylamine
* Rhynchophylline
* Sesamodil
* Silperisone
* Sipatrigine
* Terodiline
* Tetrandrine
* Tolperisone
* Trimethadione
* Valperinol

|

Activators|

* L-type-selective: Bay K8644

Potassium|

| VGKCs|

| Blockers|

* 3,4-Diaminopyridine (amifampridine)
* 4-Aminopyridine (fampridine/dalfampridine)
* Adekalant
* Almokalant
* Amiodarone
* Azimilide
* Bretylium
* Bunaftine
* Charybdotoxin
* Clamikalant
* Conotoxins
* Dalazatide
* Dendrotoxin
* Dofetilide
* Dronedarone
* E-4031
* Hanatoxin
* HgeTx1
* HsTx1
* Ibutilide
* Inakalant
* Kaliotoxin
* Linopirdine
* Lolitrem B
* Maurotoxin
* Nifekalant
* Notoxin
* Paxilline
* Pinokalant
* Quinidine
* ShK-186
* Sotalol
* Tedisamil
* Terikalant
* Tetraethylammonium
* Vernakalant

* hERG (KCNH2, Kv11.1)-specific: Ajmaline
* Amiodarone
* AmmTX3
* Astemizole
* Azaspiracid
* AZD1305
* Azimilide
* Bedaquiline
* BeKm-1
* BmTx3
* BRL-32872
* Chlorpromazine
* Cisapride
* Clarithromycin
* Darifenacin
* Dextropropoxyphene
* Diallyl trisulfide
* Domperidone
* E-4031
* Ergtoxins
* Erythromycin
* Gigactonine
* Haloperidol
* Ketoconazole
* Norpropoxyphene
* Orphenadrine
* Pimozide
* PNU-282,987
* Promethazine
* Quinidine
* Ranolazine
* Roxithromycin
* Sertindole
* Solifenacin
* Tamulotoxin
* Terodiline
* Terfenadine
* Thioridazine
* Tolterodine
* Vanoxerine
* Vernakalant

* KCNQ (Kv7)-specific: Linopirdine
* XE-991
* Spooky toxin (SsTx)

|

Activators|

* KCNQ (Kv7)-specific: Flupirtine
* Retigabine

IRKs|

| Blockers|

* KATP-specific: Acetohexamide
* Carbutamide
* Chlorpropamide
* Glibenclamide (glyburide)
* Glibornuride
* Glicaramide
* Gliclazide
* Glimepiride
* Glipizide
* Gliquidone
* Glisoxepide
* Glyclopyramide
* Glycyclamide
* Metahexamide
* Mitiglinide
* Nateglinide
* Repaglinide
* Tolazamide
* Tolbutamide

* GIRK-specific: Barium
* Caramiphen
* Cloperastine
* Clozapine
* Dextromethorphan
* Ethosuximide
* Ifenprodil
* Tertiapin
* Tipepidine

|

Activators|

* KATP-specific: Aprikalim
* Bimakalim
* Cromakalim
* Diazoxide
* Emakalim
* Levcromakalim
* Mazokalim
* Minoxidil
* Naminidil
* Nicorandil
* Pinacidil
* Rilmakalim
* Sarakalim

* GIRK-specific: ML-297 (VU0456810)

KCa|

| Blockers|

* BKCa-specific: Ethanol (alcohol)
* GAL-021

|

Activators|

* BKCa-specific: Flufenamic acid
* Meclofenamic acid
* Niflumic acid
* Nimesulide
* Rottlerin (mallotoxin)
* Tolfenamic acid

K2Ps|

| Blockers|

* 12-O-Tetradecanoylphorbol-13-acetate
* Arachidonic acid
* Fluoxetine
* Norfluoxetine

|

Activators|

* Riluzole

Sodium|

| VGSCs|

| Blockers|

* Antianginals: Ranolazine

* Antiarrhythmics (class I): Ajmaline
* Aprindine
* Disopyramide
* Dronedarone
* Encainide
* Flecainide
* Lidocaine
* Lorajmine
* Lorcainide
* Mexiletine
* Moricizine
* Pilsicainide
* Prajmaline
* Procainamide
* Propafenone
* Quinidine
* Sparteine
* Tocainide

* Anticonvulsants: Acetylpheneturide
* Carbamazepine
* Cenobamate
* Chlorphenacemide
* Elpetrigine
* Eslicarbazepine acetate
* Ethotoin
* Fosphenytoin
* Lacosamide
* Licarbazepine
* Mephenytoin
* Oxcarbazepine
* Oxitriptyline
* Phenacemide
* Pheneturide
* Phenytoin
* Rufinamide
* Sipatrigine
* Topiramate
* Sodium valproate
* Valnoctamide
* Valproate pivoxil
* Valproate semisodium
* Valproic acid
* Valpromide
* Zonisamide

* Local anesthetics: pFBT
* Amylocaine
* Articaine
* Benzocaine
* Bupivacaine (Levobupivacaine, Ropivacaine)
* Butacaine
* Butamben
* Chloroprocaine
* Cinchocaine
* Cocaine
* Cyclomethycaine
* Dimethocaine
* Diphenhydramine
* Etidocaine
* Hexylcaine
* Iontocaine
* Lidocaine
* Mepivacaine
* Meprylcaine
* Metabutoxycaine
* Orthocaine
* Piperocaine
* Prilocaine
* Procaine
* Propoxycaine
* Proxymetacaine
* Risocaine
* Tetracaine
* Trimecaine

* Analgesics: AZD-3161
* DSP-2230
* Funapide
* GDC-0276
* NKTR-171
* PF-04531083
* PF-05089771
* Ralfinamide
* Raxatrigine
* RG7893 (GDC-0287)

* Toxins: Conotoxins
* Neosaxitoxin
* Saxitoxin
* Tetrodotoxin
* Zetekitoxin AB

* Others: Buprenorphine
* Evenamide
* Menthol (mint)
* Safinamide
* Tricyclic antidepressants

|

Activators|

* Aconitine
* Atracotoxins (ω-Atracotoxin, Robustoxin, Versutoxin)
* Batrachotoxin
* Ciguatoxins
* Grayanotoxins
* Poneratoxin

ENaC|

| Blockers|

* Amiloride
* Benzamil
* Triamterene

|

Activators|

* Solnatide

ASICs|

| Blockers|

* A-317567
* Amiloride
* Aspirin
* Ibuprofen
* PcTX1

|

Chloride|

| CaCCs|

| Blockers|

* Crofelemer
* DIDS
* Ethacrynic acid
* Flufenamic acid
* Fluoxetine
* Furosemide
* Glibenclamide
* Mefloquine
* Mibefradil
* Niflumic acid

|

Activators|

* Carbachol

CFTR|

| Blockers|

* Glibenclamide
* Lonidamine
* Piretanide

|

Activators|

* 1,7-Phenanthroline
* 1,10-Phenanthroline
* 4,7-Phenanthroline
* 7,8-Benzoquinoline
* Ivacaftor
* Phenanthridine

Unsorted|

| Blockers|

* Bumetanide
* Flufenamic acid
* Meclofenamic acid
* Mefenamic acid
* Mepacrine
* Niflumic acid
* Talniflumate
* Tolfenamic acid
* Trifluoperazine

|

Others|

| TRPs|

* See here instead.

|

LGICs|

* See here instead.

See also: Receptor/signaling modulators • Transient receptor potential channel modulators

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Original source: https://en.wikipedia.org/wiki/GABA analogue. Read more

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Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:GABA_analogue&oldid=4433274"
*[GABA]: γ-Aminobutyric acid
*[GABAA]: γ-Aminobutyric acid A receptor
*[GABAA-ρ]: γ-Aminobutyric acid A-rho receptor
*[GABAB]: γ-Aminobutyric acid B receptor
*[v]: View this template
*[t]: Discuss this template
*[e]: Edit this template
*[GHB]: γ-Hydroxybutyric acid
*[GHBR]: GHB receptor
*[MCTs]: Monocarboxylate transporters
*[SMCTs]: Sodium-coupled monocarboxylate transporters
*[VIATT]: Vesicular inhibitory amino acid transporter
*[SSR]: Succinic semialdehyde reductase
*[GHBDH]: 4-Hydroxybutyrate dehydrogenase
*[HOT]: Hydroxyacid-oxoacid transhydrogenase
*[ADH]: Alcohol dehydrogenase
*[ALDH]: Aldehyde dehydrogenase
*[VDCCs]: Voltage-dependent calcium channels
*[VGKCs]: Voltage-gated potassium channels
*[IRKs]: Inwardly rectifying potassium channel
*[KATP]: ATP-sensitive potassium channel
*[GIRK]: G protein-coupled inwardly-rectifying potassium channel
*[KCa]: Calcium-activated potassium channel
*[K2Ps]: Tandem pore domain potassium channel
*[VGSCs]: Voltage-gated sodium channels
*[ENaC]: Epithelial sodium channel
*[ASICs]: Acid-sensing ion channel
*[CaCCs]: Calcium-activated chloride channel
*[CFTR]: Cystic fibrosis transmembrane conductance regulator
*[TRPs]: Transient receptor potential channels
*[LGICs]: Ligand gated ion channels