Chemistry:Ro4938581
From HandWiki
Short description: Chemical compound
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| Formula | C13H8BrF2N5 |
| Molar mass | 352.143 g·mol−1 |
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Ro4938581 is a nootropic drug invented in 2009 by a team working for Hoffmann-La Roche, which acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor. It has good selectivity for the α5 subtype and did not produce convulsant or anxiogenic effects in animal studies, making it a promising potential nootropic.[1][2][3] Ro4938581 and a related derivative basmisanil (RG-1662, RO5186582) have subsequently been investigated for the alleviation of cognitive dysfunction in Down syndrome.[4][5]
See also
References
- ↑ "RO4938581, a novel cognitive enhancer acting at GABAA alpha5 subunit-containing receptors". Psychopharmacology 202 (1–3): 207–23. January 2009. doi:10.1007/s00213-008-1357-7. PMID 18936916.
- ↑ "The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction". Bioorganic & Medicinal Chemistry Letters 19 (20): 5940–4. October 2009. doi:10.1016/j.bmcl.2009.08.053. PMID 19762240.
- ↑ "Negative modulation of GABAA α5 receptors by RO4938581 attenuates discrete sub-chronic and early postnatal phencyclidine (PCP)-induced cognitive deficits in rats". Psychopharmacology 221 (3): 451–68. June 2012. doi:10.1007/s00213-011-2593-9. PMID 22124672.
- ↑ "Reducing GABAA α5 receptor-mediated inhibition rescues functional and neuromorphological deficits in a mouse model of down syndrome". The Journal of Neuroscience 33 (9): 3953–66. February 2013. doi:10.1523/JNEUROSCI.1203-12.2013. PMID 23447605.
- ↑ Breindl, Anette (2019). "Inhibiting Inhibition to Treat Down Syndrome Symptoms". BioWorld. http://www.bioworld.com/content/inhibiting-inhibition-treat-down-syndrome-symptoms-1.
{{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 =
| below =
- See also
- Receptor/signaling modulators
- GABAA receptor positive modulators
- GABA metabolism/transport modulators
}}
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