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125 results
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Page 1
The modulatory action of loreclezole at the gamma-aminobutyric acid type A receptor is determined by a single amino acid in the beta 2 and beta 3 subunit.
Wingrove PB, Wafford KA, Bain C, Whiting PJ. Wingrove PB, et al. Proc Natl Acad Sci U S A. 1994 May 10;91(10):4569-73. doi: 10.1073/pnas.91.10.4569. Proc Natl Acad Sci U S A. 1994. PMID: 8183949 Free PMC article.
The action of loreclezole depends on the type of beta subunit present in the receptor complex; receptors containing beta 2 or beta 3 subunits have > 300-fold higher affinity for loreclezole than receptors containing a beta 1 subunit. ...By mutating single amino a …
The action of loreclezole depends on the type of beta subunit present in the receptor complex; receptors containing beta 2 or beta 3 …
Loreclezole inhibition of recombinant alpha1beta1gamma2L GABA(A) receptor single channel currents.
Fisher JL, Hinkle DJ, Macdonald RL. Fisher JL, et al. Neuropharmacology. 2000 Jan 4;39(2):235-45. doi: 10.1016/s0028-3908(99)00108-2. Neuropharmacology. 2000. PMID: 10670419
Loreclezole had two different effects on GABA(A) receptor (GABAR) currents. ...Loreclezole also increased the occurrence of a closed component with an average duration near 20 ms. ...
Loreclezole had two different effects on GABA(A) receptor (GABAR) currents. ...Loreclezole also increased the occurrence of a …
Direct activation of GABAA receptors by loreclezole, an anticonvulsant drug with selectivity for the beta-subunit.
Sanna E, Murgia A, Casula A, Usala M, Maciocco E, Tuligi G, Biggio G. Sanna E, et al. Neuropharmacology. 1996;35(12):1753-60. doi: 10.1016/s0028-3908(96)00138-4. Neuropharmacology. 1996. PMID: 9076754
At 100 microM, the current evoked by loreclezole was 26% of that induced by 5 microM GABA. The current evoked by 100 microM propofol was 98% of that induced by 5 microM GABA. ...The failure of loreclezole to activate GABAA receptors containing the beta 1-subunit may …
At 100 microM, the current evoked by loreclezole was 26% of that induced by 5 microM GABA. The current evoked by 100 microM propofol …
Synthesis of trans N-Substituted Pyrrolidine Derivatives Bearing 1,2,4- triazole Ring.
Prasad TN, Reddy YP, Settipalli PC, Kumar VS, Reddy EK, Basha SF, Anwar S. Prasad TN, et al. Curr Org Synth. 2022 Aug 6;19(5):578-582. doi: 10.2174/1570179419666211230094334. Curr Org Synth. 2022. PMID: 34967296
OBJECTIVE: The core motif of 1,2,4-triazoles plays a vital role in clinical drugs such as Rizatriptan (antimigraine), Ribavirin (antiviral), anastrozole (anticancer), etizolam (anxiolytic), estazolam (anticonvulsant), alprazolam (anti-hypnotic), letrozole (aromatase inhibitor), …
OBJECTIVE: The core motif of 1,2,4-triazoles plays a vital role in clinical drugs such as Rizatriptan (antimigraine), Ribavirin (antiviral), …
Pharmacodynamic and/or pharmacokinetic characteristics of interactions between loreclezole and four conventional antiepileptic drugs in pentylenetetrazole-induced seizures in mice: an isobolographic analysis.
Luszczki JJ, Ratnaraj N, Patsalos PN, Czuczwar SJ. Luszczki JJ, et al. Epilepsy Behav. 2005 Dec;7(4):639-51. doi: 10.1016/j.yebeh.2005.07.007. Epub 2005 Sep 2. Epilepsy Behav. 2005. PMID: 16140589
Isobolographic analysis was used to characterize the interactions between loreclezole (LCZ) and clonazepam (CZP), ethosuximide (ETS), phenobarbital (PB), and valproate (VPA) in suppressing pentylenetetrazole (PTZ)-induced seizures and in producing acute neurotoxic adverse …
Isobolographic analysis was used to characterize the interactions between loreclezole (LCZ) and clonazepam (CZP), ethosuximide (ETS), …
In vivo studies on the mechanism of action of the broad spectrum anticonvulsant loreclezole.
Ashton D, Fransen J, Heeres J, Clincke GH, Janssen PA. Ashton D, et al. Epilepsy Res. 1992 Mar;11(1):27-36. doi: 10.1016/0920-1211(92)90018-o. Epilepsy Res. 1992. PMID: 1563336
The decrease in the duration of forepaw clonus and the reduction in behavioural stage34 produced by loreclezole, pentobarbital and diazepam was reversed by CGS-8216. Ro-15-1788, which itself showed anticonvulsant effects in this model, antagonized the effects of diazepam, …
The decrease in the duration of forepaw clonus and the reduction in behavioural stage34 produced by loreclezole, pentobarbital and di …
Novel alpha6 preferring GABA-A receptor ligands based on loreclezole.
Simeone X, Ernst M, Seidel T, Heider J, Enz D, Monticelli S, Vogel FD, Koniuszewski F, Langer T, Scholze P, Pace V, Miele M. Simeone X, et al. Eur J Med Chem. 2022 Dec 15;244:114780. doi: 10.1016/j.ejmech.2022.114780. Epub 2022 Sep 17. Eur J Med Chem. 2022. PMID: 36279694
The subunit encoded by the GABRA6 gene is highly expressed in the cerebellum and the receptors to which it contributes have recently been demonstrated to be a promising candidate as a novel drug target. Here we examined a series of loreclezole derivatives for potentially s …
The subunit encoded by the GABRA6 gene is highly expressed in the cerebellum and the receptors to which it contributes have recently been de …
Interaction of loreclezole with conventional antiepileptic drugs in amygdala-kindled rats.
Borowicz KK, Sawiniec A, Czuczwar SJ. Borowicz KK, et al. Eur Neuropsychopharmacol. 2004 May;14(3):251-7. doi: 10.1016/j.euroneuro.2003.09.004. Eur Neuropsychopharmacol. 2004. PMID: 15056485
Although, loreclezole significantly increased the free plasma concentration of carbamazepine. The results point to the potential therapeutic effects of combinations of loreclezole with valproate or clonazepam....
Although, loreclezole significantly increased the free plasma concentration of carbamazepine. The results point to the potential ther …
Topiramate modulation of β(1)- and β(3)-homomeric GABA(A) receptors.
Simeone TA, Wilcox KS, White HS. Simeone TA, et al. Pharmacol Res. 2011 Jul;64(1):44-52. doi: 10.1016/j.phrs.2011.03.004. Epub 2011 Mar 21. Pharmacol Res. 2011. PMID: 21421049
Similar to picrotoxin, application of topiramate, pentobarbital and loreclezole inhibited beta(1)-homomers. In contrast, these compounds activated beta(3)-homomers. ...Interaction studies suggested competition between topiramate, loreclezole and pentobarbital for ac …
Similar to picrotoxin, application of topiramate, pentobarbital and loreclezole inhibited beta(1)-homomers. In contrast, these compou …
Interactions between loreclezole, chlormethiazole and pentobarbitone at GABA(A) receptors: functional and binding studies.
Zhong Y, Simmonds MA. Zhong Y, et al. Br J Pharmacol. 1997 Aug;121(7):1392-6. doi: 10.1038/sj.bjp.0701269. Br J Pharmacol. 1997. PMID: 9257919 Free PMC article.
A small component of the enhancement by loreclezole could be blocked by 100 microM bicuculline and could also be blocked by 100 microM chlormethiazole. ...The results indicate distinctly different profiles of action for loreclezole, chlormethiazole and pentobarbiton …
A small component of the enhancement by loreclezole could be blocked by 100 microM bicuculline and could also be blocked by 100 micro …
125 results