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Chemical Compound Review

saclofen     3-amino-2-(4- chlorophenyl)propane-1...

Synonyms: CHEMBL312403, ANW-45829, CHEBI:226133, BPBio1_000705, AK-86940, ...
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Disease relevance of saclofen

  • 3. The effect of anoxia was not blocked by tetrodotoxin (TTX), saclofen, (-)sulpiride, or strychnine [1].
  • The sensitivity of DRG neurones to gabapentin was not changed by the GABA(B) receptor antagonist saclofen but pertussis toxin pre-treatment reduced the inhibitory effects of gabapentin [2].
  • Desipramine (20 mg/kg, i.p.) significantly blocked the adjuvant-induced thermal hyperalgesia, which was facilitated by treatment with the GABA(A) antagonist picrotoxin (2 mg/kg, i.p.) or the GABA(B) antagonist saclofen (2 mg/kg, i.p.). This analgesic effect of desipramine was antagonized by post-treatment with picrotoxin or saclofen [3].

High impact information on saclofen

  • 2-OH Saclofen, a GABAB receptor antagonist, prevented the reduction of inhibition, the increase of excitation, and the induction of LTP [4].
  • Bicuculline, but not saclofen, induced a large and prompt increase in LHRH release in prepubertal monkeys, whereas it stimulated LHRH release slightly in pubertal monkeys [5].
  • Muscimol-induced feeding was blocked by coadministration of the selective GABAA receptor blocker bicuculline, but not by the GABAB receptor blocker saclofen [6].
  • Micromolar levels of both molecules stimulated cell migration that was blocked by micromolar saclofen [7].
  • This secondary effect of nicotine was blocked by a combination of picrotoxin (50 microM) and saclofen (100 microM), and thus appeared to be mediated via GABAergic interneurons [8].

Biological context of saclofen

  • The selective GABA(B) receptor antagonist saclofen (0.1 mM) completely blocked the effect of (-)-baclofen on VLC EPSP [9].
  • The oscillation was insensitive to the bath application of a combination of blockers to excitatory and inhibitory synaptic transmission, including 30 microM 6,7-dinitroquinoxaline-2,3-dione, 100 microM (+/-)-2-amino-5-phosphonopentanoic acid, 20 microM bicuculline, and 2 mM saclofen, suggesting an intrinsic event [10].
  • Intrastriatal infusion of malonate (2 micromol) plus or minus the GABA(A) receptor agonist muscimol (1 micromol), the GABA(A) Cl- binding site antagonist picrotoxin (50 nmol) or the GABA(B) receptor antagonist saclofen (33 nmol) did not modify loss of striatal dopamine or GABA when examined 1 week following infusion [11].
  • Neither bicuculline nor saclofen in the nucleus accumbens shell altered baseline food intake [12].
  • Saclofen reversed the action of (+/-)-baclofen, 50 microM, with a half maximal inhibitory concentration (IC50) of about 1.0 mM [13].

Anatomical context of saclofen

  • Using the tracheal preparations, the effects of GABA and GABAa and GABAb receptor agonists (muscimol and baclofen) and antagonists (bicuculline and saclofen) on the basal tone of the trachea and on tracheal contraction induced by electrical field stimulation (EFS) were determined [14].
  • In contrast, mu opioid agonist-induced feeding elicited from the nucleus accumbens shell was dose-dependently decreased by GABA(B) (saclofen) antagonism [12].
  • Picrotoxin alone did not have any effect on the acrosome reaction induced by the FF, whereas it had a significant suppressive effect if coincubated with saclofen [15].
  • Adult male Sprague-Dawley rats were implanted with cannulae directed to the rostral lateral hypothalamus and saclofen (GABA-B receptor antagonist), biccuculine (GABA-A receptor antagonist) or muscimol (GABA-A receptor agonist) were injected prior to orexin A [16].
  • DAMGO-induced feeding elicited from the ventral tegmental area (VTA) region is significantly reduced by pretreatment with saclofen into the same site indicating local GABA mediation of opioid-induced feeding in each site [17].

Associations of saclofen with other chemical compounds

  • The GABAB receptor ligands baclofen, phaclofen, and saclofen (1-100 microM) had no appreciable effects on the rho-like receptors [18].
  • 4. The amplitude of the late, GABAB receptor-mediated inhibitory postsynaptic potential (i.p.s.p.) was reduced by the GABAB antagonists as follows (means +/- s.e.mean): CGP 55845A (1 microM) 91 +/- 5%, CGP 52432 (1 microM) 64 +/- 5%, CGP 35348 (100 microM) 82 +/- 5%, CGP 36742 (100 microM) 76 +/- 8%, and 2-OH saclofen (100 microM) 68 +/- 3% [19].

Gene context of saclofen

  • The effect of a maximally effective concentration of FF (30%, vol/vol) was significantly suppressed by bicuculline, a GABAA receptor antagonist, and saclofen, a GABAB receptor antagonist, added concomitantly [15].
  • LTDi was mediated by activation of a presynaptic GABAB receptor, because it was blocked by saclofen and CGP55845 [(2S)-3-{[(15)-1-(3, 4-dichlorophenyl)ethyl]amino-2-hydroxypropyl)(phenylmethyl)phosphinic acid] [20].
  • 5. On the other hand, the cardiovascular depressive responses to blockade of endogenous nNOS activity were significantly antagonized on co-administration of GABA(A) receptor antagonist, bicuculline methiodine (5 or 10 pmoles), but not GABA(B) receptor antagonist, 2-hydroxy saclofen (50 or 100 pmoles) [21].
  • For known GABA(B) agonists the rank order was CGP27492>SKF97541=CGP46381>GABA>Baclofen and for GABA(B) antagonists the rank order was CGP54262A>CGP55845>CGP52432>SCH 50911>CGP51176>CGP36742=CGP35348 > or =2-OH Saclofen > or =ABPA [22].
  • Such olfactory aversions were observed even if saclofen was infused without odour exposure [23].

Analytical, diagnostic and therapeutic context of saclofen

  • Under bicuculline and saclofen perfusion, HFS provoked a slight potentiation of the N2 wave, while the N2 depression clearly emerged after drug wash-out [24].
  • In addition, the PBN-induced cardiac BRR suppression was reversed by microinjection bilaterally into the NTS of a GABA(A) receptor antagonist, bicuculline methiodide (5 pmol), or a GABA(B) receptor antagonist, 2-OH saclofen (500 pmol) [25].
  • Perfusion of either bicuculline methiodide, a GABA(A) receptor antagonist, or saclofen, a GABA(B) receptor antagonist, through a microdialysis probe resulted in dose-dependent increases in NO(x)(-) levels [26].
  • The GABAB receptor antagonist saclofen (3-amino-2-(4-chlorophenyl)propylsulphonic acid) has been resolved by chiral high-performance liquid chromatography [27].
  • No effect on the spontaneous firing rate was observed following iontophoresis of the selective GABA-antagonists, picrotoxin (GABA-A receptor antagonist) or saclofen (GABA-B receptor antagonist) [28].


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  15. Human follicular fluid stimulates the sperm acrosome reaction by interacting with the gamma-aminobutyric acid receptors. Burrello, N., Vicari, E., D'Amico, L., Satta, A., D'Agata, R., Calogero, A.E. Fertil. Steril. (2004) [Pubmed]
  16. Orexin A in the rostrolateral hypothalamic area induces feeding by modulating GABAergic transmission. Thorpe, A.J., Doane, D.F., Sweet, D.C., Beverly, J.L., Kotz, C.M. Brain Res. (2006) [Pubmed]
  17. Lack of intersite GABA receptor subtype antagonist effects upon mu opioid receptor agonist-induced feeding elicited from either the ventral tegmental area or nucleus accumbens shell in rats. Ackerman, T.F., Lamonte, N., Bodnar, R.J. Physiol. Behav. (2003) [Pubmed]
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  22. Characterization of [(3)H]-CGP54626A binding to heterodimeric GABA(B) receptors stably expressed in mammalian cells. Green, A., Walls, S., Wise, A., Green, R.H., Martin, A.K., Marshall, F.H. Br. J. Pharmacol. (2000) [Pubmed]
  23. Modulation of olfactory learning in young rats through intrabulbar GABA(B) receptors. Okutani, F., Zhang, J.J., Otsuka, T., Yagi, F., Kaba, H. Eur. J. Neurosci. (2003) [Pubmed]
  24. The role of GABA in NMDA-dependent long term depression (LTD) of rat medial vestibular nuclei. Grassi, S., Della Torre, G., Capocchi, G., Zampolini, M., Pettorossi, V.E. Brain Res. (1995) [Pubmed]
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