Aptiganel

Aptiganel
Aptiganel
Systematic (IUPAC) name
1-(3-ethylphenyl)-1-methyl-2-naphthalen-1-ylguanidine
Clinical data
Pregnancy cat.  ?
Legal status Uncontrolled
Identifiers
CAS number 137159-92-3
ATC code None
PubChem CID 60840
UNII 46475LV84I YesY
Chemical data
Formula C20H21N3 
Mol. mass 303.401 g/mol
SMILES eMolecules & PubChem
 YesY(what is this?)  (verify)

Aptiganel (Cerestat; CNS-1102) is a drug which acts as a noncompetitive NMDA antagonist.[1] It has neuroprotective effects and was researched for potential use in the treatment of stroke,[2] but despite positive results in animal studies,[3] human trials showed limited efficacy,[4] as well as undesirable side effects such as sedation and hallucinations,[5][6] and clinical development was ultimately not continued.[7]

Aptiganel synth.png

References

  1. ^ Reddy NL, Hu LY, Cotter RE, Fischer JB, Wong WJ, McBurney RN, Weber E, Holmes DL, Wong ST, Prasad R, et al. Synthesis and structure-activity studies of N,N'-diarylguanidine derivatives. N-(1-naphthyl)-N'-(3-ethylphenyl)-N'-methylguanidine: a new, selective noncompetitive NMDA receptor antagonist. Journal of Medicinal Chemistry. 1994 Jan 21;37(2):260-7. PMID 8295213
  2. ^ Muir KW, Grosset DG, Gamzu E, Lees KR. Pharmacological effects of the non-competitive NMDA antagonist CNS 1102 in normal volunteers. British Journal of Clinical Pharmacology. 1994 Jul;38(1):33-8. PMID 7946934
  3. ^ Schäbitz WR, Li F, Fisher M. The N-methyl-D-aspartate antagonist CNS 1102 protects cerebral gray and white matter from ischemic injury following temporary focal ischemia in rats. Stroke. 2000 Jul;31(7):1709-14. PMID 10884477
  4. ^ Albers GW, Goldstein LB, Hall D, Lesko LM; Aptiganel Acute Stroke Investigators. Aptiganel hydrochloride in acute ischemic stroke: a randomized controlled trial. Journal of the American Medical Association. 2001 Dec 5;286(21):2673-82. PMID 11730442
  5. ^ Muir KW, Grosset DG, Lees KR. Effects of prolonged infusions of the NMDA antagonist aptiganel hydrochloride (CNS 1102) in normal volunteers. Clinical Neuropharmacology. 1997 Aug;20(4):311-21. PMID 9260729
  6. ^ Lees KR. Cerestat and other NMDA antagonists in ischemic stroke. Neurology. 1997 Nov;49(5 Suppl 4):S66-9. PMID 9371155
  7. ^ Hoyte L, Barber PA, Buchan AM, Hill MD. The rise and fall of NMDA antagonists for ischemic stroke. Current Molecular Medicine. 2004 Mar;4(2):131-6. PMID 15032709




Wikimedia Foundation. 2010.

Нужно сделать НИР?

Look at other dictionaries:

  • Phencyclidine — Systematic (IUPAC) name …   Wikipedia

  • Toluene — IUPAC name …   Wikipedia

  • Nitrous oxide — N2O redirects here. For other uses, see N2O (disambiguation). Laughing gas redirects here. For other uses, see Laughing gas (disambiguation). Not to be confused with nitric oxide (formula NO) or nitrogen dioxide (formula NO2). For other uses, see …   Wikipedia

  • Dizocilpine — Systematic (IUPAC) name (+) 5 methyl 10,11 dihydro 5H dibenzo[a,d]cyclohepten 5,10 imine maleate Clinical data Pregnancy cat …   Wikipedia

  • Dextrorphan — Systematic (IUPAC) name (+) 17 methyl 9a,13a,14a morphinan 3 ol …   Wikipedia

  • Dextromethorphan — Not to be confused with Dexamethasone. Dextromethorphan Systematic (IUP …   Wikipedia

  • Methorphan — Systematic (IUPAC) name 3 methoxy 17 methylmorphinan Clinical data Pregnancy cat.  ? Legal status  ? Identifiers CAS number …   Wikipedia

  • NMDA receptor antagonist — Ketamine, one of the most common NMDA receptor antagonists. NMDA receptor antagonists are a class of anesthetics that work to antagonize, or inhibit the action of, the N methyl d aspartate receptor (NMDAR). They are used as anesthesia for animals …   Wikipedia

  • Dexoxadrol — Systematic (IUPAC) name (2S) 2 [(4S) 2,2 di(phenyl) 1,3 dioxolan 4 yl]piperidine Clinical data Pregnancy cat.  ? …   Wikipedia

  • Neramexane — Systematic (IUPAC) name 1,3,3,5,5 pentamethylcyclohexanamine Clinical data Pregnancy cat.  ? …   Wikipedia

Share the article and excerpts

Direct link
Do a right-click on the link above
and select “Copy Link”