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  1. World Encyclopedia
  2. CGP-35348 - Wikipedia
CGP-35348 - Wikipedia
From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
CGP-35348
Identifiers
IUPAC name
  • 3-Aminopropyl(diethoxymethyl)phosphinic acid
CAS Number
  • 123690-79-9 checkY
PubChem CID
  • 107699
IUPHAR/BPS
  • 1069
ChemSpider
  • 96869 ☒N
UNII
  • 87TI61875H
CompTox Dashboard (EPA)
  • DTXSID70154064 Edit this at Wikidata
Chemical and physical data
FormulaC8H20NO4P
Molar mass225.225 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • CCOC(OCC)P(=O)(CCCN)O
InChI
  • InChI=1S/C8H20NO4P/c1-3-12-8(13-4-2)14(10,11)7-5-6-9/h8H,3-7,9H2,1-2H3,(H,10,11) ☒N
  • Key:QIIVUOWTHWIXFO-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

CGP-35348 is a compound used in scientific research which acts as an antagonist at GABAB receptors.[1][2][3]

CGP-35348 was ineffective up to 100 μM to antagonize the inhibitory release of GABA elicited by baclofen, doing so selectively as a GABAB heteroreceptor antagonist. [4] Moreover, CGP-35348 was about threefold less potent in antagonizing gamma-hydroxybutyrate (GHB) and gamma-butyrolactone (GBL) than baclofen and SKF-97,541.[5]

References

[edit]
  1. ^ Carter LP, Chen W, Coop A, Koek W, France CP (May 2006). "Discriminative stimulus effects of GHB and GABA(B) agonists are differentially attenuated by CGP35348". European Journal of Pharmacology. 538 (1–3): 85–93. doi:10.1016/j.ejphar.2006.03.039. PMID 16647701.
  2. ^ Nasrallah FA, Griffin JL, Balcar VJ, Rae C (August 2007). "Understanding your inhibitions: modulation of brain cortical metabolism by GABA(B) receptors". Journal of Cerebral Blood Flow and Metabolism. 27 (8): 1510–20. doi:10.1038/sj.jcbfm.9600453. PMID 17293844. S2CID 16069846.
  3. ^ Koek W, Mercer SL, Coop A, France CP (September 2009). "Behavioral effects of gamma-hydroxybutyrate, its precursor gamma-butyrolactone, and GABA(B) receptor agonists: time course and differential antagonism by the GABA(B) receptor antagonist 3-aminopropyl(diethoxymethyl)phosphinic acid (CGP35348)". The Journal of Pharmacology and Experimental Therapeutics. 330 (3): 876–83. doi:10.1124/jpet.109.151845. PMC 2729800. PMID 19564487.
  4. ^ Maurizio Raiteri (2006). "Functional Pharmacology in Human Brain". Pharmacological Reviews. 58 (2): 162–193. doi:10.1124/pr.58.2.5. PMID 16714485. S2CID 14404544.
  5. ^ Koek W1, Mercer SL, Coop A. (June 2007). "Cataleptic effects of gamma-hydroxybutyrate (GHB), its precursor gamma-butyrolactone (GBL), and GABAB receptor agonists in mice: differential antagonism by the GABAB receptor antagonist CGP35348". Psychopharmacology. 192 (3): 407–14. doi:10.1007/s00213-007-0718-y. PMID 17277933. S2CID 25049526.{{cite journal}}: CS1 maint: multiple names: authors list (link) CS1 maint: numeric names: authors list (link)
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GABA receptor modulators
Ionotropic
GABAATooltip γ-Aminobutyric acid A receptor
  • Agonists: 4-AHP
  • (+)-Catechin
  • Bamaluzole
  • Barbiturates (e.g., phenobarbital)
  • Beta-Alanine
  • BL-1020
  • DAVA
  • DH-P4S
  • Dihydromuscimol
  • GABA
  • Gabamide
  • GABOB
  • Gaboxadol (THIP)
  • Homotaurine (tramiprosate, 3-APS)
  • IAA (IMA)
  • Ibotenic acid
  • iso-THAZ
  • Isoguvacine
  • Isonipecotic acid
  • Kojic amine
  • L-838,417
  • Lignans (e.g., honokiol)
  • Methylglyoxal
  • Monastrol
  • Muscimol
  • Nefiracetam
  • Neuroactive steroids (e.g., allopregnanolone)
  • Org 20599
  • PF-6372865
  • Phenibut
  • Picamilon
  • 4-PIOL
  • P4S
  • Progabide
  • Propofol
  • Quisqualamine
  • SL-75102
  • Taurine
  • TACA
  • TAMP
  • Terpenoids (e.g., borneol)
  • Thio-4-PIOL
  • Thiomuscimol
  • Tolgabide
  • ZAPA
  • 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)
  • Antagonists: Bicuculline
  • Coriamyrtin
  • Dihydrosecurinine
  • Famiraprinium
  • Gabazine (SR-95531)
  • Hydrastine
  • Hyenanchin (mellitoxin)
  • Iso-THIP
  • PHP-501
  • Pitrazepin
  • Securinine
  • Sinomenine
  • SR-42641
  • THAZ
  • Thio-4-PIOL
  • Thio-THIP
  • Thiocolchicoside
  • Tutin
  • 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
  • Bupleurotoxin
  • 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
  • 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)
  • PNV-001
  • 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-ρTooltip γ-Aminobutyric acid A-rho receptor
  • 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
  • Aza-THIP
  • CGP-36742 (SGS-742)
  • DAVA
  • Gabazine (SR-95531)
  • Gaboxadol (THIP)
  • I4AA
  • Iso-THIP
  • Isonipecotic acid
  • Loreclezole
  • P4MPA
  • P4S
  • SKF-97541
  • SR-95318
  • SR-95813
  • THAZ
  • Thio-THIP
  • TPMPA
  • trans-3-ACPBPA
  • ZAPA
  • Negative modulators: 5α-Dihydroprogesterone
  • Bilobalide
  • Loreclezole
  • Picrotoxin (picrotin, picrotoxinin)
  • Pregnanolone
  • ROD-188
  • THDOC
  • Zinc
Metabotropic
GABABTooltip γ-Aminobutyric acid B receptor
  • Agonists: 1,4-Butanediol
  • 3-APPA
  • 4-Fluorophenibut
  • Aceburic acid
  • Arbaclofen
  • Arbaclofen placarbil
  • Baclofen
  • BL-1020
  • GABA
  • Gabamide
  • GABOB
  • GBL
  • GHB
  • GHBAL
  • GHV
  • GVL
  • Isovaline
  • JZP-386
  • Lesogaberan
  • Phenibut
  • Picamilon
  • Progabide
  • Sodium oxybate
  • SKF-97,541
  • SL 75102
  • Tolgabide
  • Tolibut
  • Valiloxybate (XW-10172)
  • Positive modulators: ADX-71441
  • ASP-8062
  • BHF-177
  • BHFF
  • rac-BHFF
  • BSPP
  • CGP-7930
  • CGP-13501
  • GS-39783
  • INDV-1000
  • KK-92A
  • Antagonists: 2-Hydroxysaclofen
  • CGP-35348
  • CGP-36742
  • CGP-46381
  • CGP-52432
  • CGP-54626
  • CGP-55845
  • CGP-64213
  • DAVA
  • Homotaurine (tramiprosate, 3-APS)
  • Phaclofen
  • Saclofen
  • SCH-50911
  • Negative modulators: Compound 14
See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators


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