FG-7142
FG-7142
Names
Preferred IUPAC name
N -Methyl-5H -pyrido[3,4-b ]indole-2-carboxamide
Other names
ZK-31906
Identifiers
ChemSpider
MeSH
C526324
UNII
InChI=1S/C13H11N3O/c1-14-13(17)11-6-9-8-4-2-3-5-10(8)16-12(9)7-15-11/h2-7,16H,1H3,(H,14,17)
N Key: QMCOPDWHWYSJSA-UHFFFAOYSA-N
N
CNC(=O)C1=NC=C2C(=C1)C3=CC=CC=C3N2
Properties
C13 H11 N3 O
Molar mass
225.24594
Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
Chemical compound
FG-7142 (ZK-31906 ) is a drug which acts as a partial inverse agonist at the benzodiazepine allosteric site of the GABAA receptor .[ 1] It has anorectic ,[ 2] anxiogenic and pro-convulsant effects.[ 3] It also increases release of acetylcholine and noradrenaline ,[ 4] and improves memory retention in animal studies.[ 5]
References
^ Stevenson CW, Halliday DM, Marsden CA, Mason R (2007). "Systemic administration of the benzodiazepine receptor partial inverse agonist FG-7142 disrupts corticolimbic network interactions". Synapse . 61 (8): 646–63. CiteSeerX 10.1.1.323.5370 . doi :10.1002/syn.20414 . PMID 17503486 . S2CID 13415418 .
^ Cottone P, Sabino V, Steardo L, Zorrilla EP (May 2007). "FG 7142 specifically reduces meal size and the rate and regularity of sustained feeding in female rats: evidence that benzodiazepine inverse agonists reduce food palatability" . Neuropsychopharmacology . 32 (5): 1069–81. doi :10.1038/sj.npp.1301229 . PMID 17077811 .
^ Evans AK, Lowry CA (Winter 2007). "Pharmacology of the β-carboline FG-7142, a partial inverse agonist at the benzodiazepine allosteric site of the GABAA receptor: neurochemical, neurophysiological, and behavioral effects" . CNS Drug Reviews . 13 (4): 475–501. doi :10.1111/j.1527-3458.2007.00025.x . PMC 6494137 . PMID 18078430 .
^ Claustre Y, Rouquier L, Desvignes C, Leonetti M, Montégut J, Aubin N, Allouard N, Bougault I, Oury-Donat F, Steinberg R (2006). "Effects of the vasopressin (V1b) receptor antagonist, SSR149415, and the corticotropin-releasing factor 1 receptor antagonist, SSR125543, on FG 7142-induced increase in acetylcholine and norepinephrine release in the rat". Neuroscience . 141 (3): 1481–8. doi :10.1016/j.neuroscience.2006.05.006 . PMID 16781820 . S2CID 24944657 .
^ McNally GP, Augustyn KA, Richardson R (2008). "GABAA receptors determine the temporal dynamics of memory retention" . Learning and Memory . 15 (3): 106–11. doi :10.1101/lm.806008 . PMC 2275652 . PMID 18285469 .
Ionotropic
GABAA Tooltip γ-Aminobutyric acid A receptor
Positive modulators (abridged; see here for a full list): α-EMTBL
Alcohols (e.g., drinking alcohol , 2M2B )
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 )
Lanthanum
Loreclezole
Monastrol
Neuroactive steroids (e.g., allopregnanolone , cholesterol , THDOC )
Niacin
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 , diethyl ether , paraldehyde , sevoflurane )
Negative modulators: 1,3M1B
3M2B
11-Ketoprogesterone
17-Phenylandrostenol
α3IA
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 (123 I)
IPTBO
Isopregnanolone (sepranolone)
L-655,708
Laudanosine
Lindane
MaxiPost
Morphine
Morphine-3-glucuronide
MRK-016
Naloxone
Naltrexone
Nicardipine
Nonsteroidal antiandrogens (e.g., apalutamide , bicalutamide , enzalutamide , flutamide , 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
GABAA -ρ Tooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABAB Tooltip γ-Aminobutyric acid B receptor