Protein Information

Name benzodiazepine receptor (protein family or complex)
Synonyms Benzodiazepine receptor; benzodiazepine (BDZ) receptor; BDZ receptor

Compound Information

Name strychnine
CAS strychnidin-10-one

Reference List

PubMed Abstract RScore(About this table)
8539344 Molewijk HE, van der Poel AM, Olivier B: The ambivalent behaviour "stretched approach posture" in the rat as a paradigm to characterize anxiolytic drugs. Psychopharmacology. 1995 Sep;121(1):81-90.

Finally, the 5-HT2C receptor antagonist ritanserine, the CCKA receptor antagonist devazepide, the CCKB receptor antagonist L-365.260 and the strychnine-insensitive glycine site antagonist 7-Cl-kynurenic acid were without effect on the behaviours in this paradigm using single doses.
The benzodiazepine receptor agonists chlordiazepoxide, diazepam and alprazolam, the 5-HT1A receptor agonists flesinoxan and ipsapirone and the 5-HT uptake inhibitor clomipramine selectively (no effect on crossings) reduced SAP.
2(0,0,0,2) Details
9895039 Kostowski W, Bienkowski P: Discriminative stimulus effects of ethanol: neuropharmacological characterization. Alcohol. 1999 Jan;17(1):63-80.

Substitution studies have shown that the complete substitution for ethanol may be exerted by certain GABA-mimetic drugs acting through different sites within the GABA (A)-benzodiazepine receptor complex (e.g., diazepam, pentobarbital, certain neurosteroids), gamma-hydroxybutyrate, and antagonists of the glutamate NMDA receptor.
Further, some antagonists of strychnine-insensitive glycine modulatory sites among the NMDA receptor complex (e.g., L-701,324) dose-dependently substitute for the ethanol discriminative stimulus.
2(0,0,0,2) Details
11952420 Menzikov SA, Menzikova OV: Effect of activators and blockers of ligand-regulated ion channels on the activity of the Cl-stimulated Mg2+-ATPase of the plasma membrane fraction from bream (Abramis brama L.) brain. Biochemistry. 2002 Feb;67(2):233-9.

The activation of "basal" Mg (2+)-ATPase by neuromediators was decreased by blockers of the corresponding receptors (picrotoxin, strychnine, benztropine mesylate, and D-2-amino-5-phosphonovaleric acid).
Agonists of the GABAa/benzodiazepine receptor--phenazepam (10 (-8)-10 (-4) M) and pentobarbital (10 (-6)-10 (-3) M)--activated the "basal" Mg (2+)-ATPase activity and decreased the Cl (-)-stimulated Mg (2+)-ATPase activity.
1(0,0,0,1) Details
15056857 Koo BS, Lee SI, Ha JH, Lee DU: Inhibitory effects of the essential oil from SuHeXiang Wan on the central nervous system after inhalation. Biol Pharm Bull. 2004 Apr;27(4):515-9.

Preinhalation of the fragrance oil markedly delayed the appearance of pentylenetetrazole-induced convulsion, but showed weak activities on picrotoxin- and strychnine-induced convulsions, which implies this drug may inhibit the convulsion by GABAergic neuromodulation.
This essential oil inhibited the binding of [(3) H] Ro15-1788, a selective antagonist for the benzodiazepine receptor and also the binding of [(3) H] flunitrazepam, a selective agonist for the receptor, in the presence of gamma-aminobutyric acid (GABA) and NaCl, showing a positive GABA shift, which suggested the strong possibility of the agonistic activity of the essential oil to the GABA/benzodiazepine receptor complex in rat cerebral cortices.
1(0,0,0,1) Details
7834364 Drugan RC, Basile AS, Ha JH, Ferland RJ: The protective effects of stress control may be mediated by increased brain levels of benzodiazepine receptor agonists. Brain Res. 1994 Oct 24;661(1-2):127-36.

1(0,0,0,1) Details
8813615 Zhao TJ, Rosenberg HC, Chiu TH: Treatment with an antisense oligodeoxynucleotide to the GABAA receptor gamma 2 subunit increases convulsive threshold for beta-CCM, a benzodiazepine "inverse agonist', in rats. Eur J Pharmacol. 1996 Jun 13;306(1-3):61-6.

Both antisense and sense oligodeoxynucleotide treatments slightly increased the threshold for strychnine seizures.
The results suggest that antisense oligodeoxynucleotide treatment altered GABAA receptor composition and interfered with the actions of a benzodiazepine receptor ligand in vivo, and may provide a tool for studying regulation of receptor structure and function.
1(0,0,0,1) Details
9004347 Kawasaki K, Eigyo M, Ikeda M, Kihara T, Koike K, Matsushita A, Murata S, Shiomi T, Takada S, Yasui M: A novel benzodiazepine inverse agonist, S-8510, as a cognitive enhancer. Prog Neuropsychopharmacol Biol Psychiatry. 1996 Nov;20(8):1413-25.

Pharmacological actions of a novel benzodiazepine receptor ligand, S-8510 (2-(3-isoxazolyl)-3,6,7,9-tetrahydroimidazo [4,5-d] pyrano+ ++[4,3-b] pyridine monophosphate monohydrate), were examined in in vitro and in vivo studies. 2.
S-8510 selectively potentiated pentylenetetrazol-induced convulsion without affecting minimal electroconvulsive shock- or strychnine-induced convulsion in ddY mice. 7.
1(0,0,0,1) Details
12659934 Trapani G, Latrofa A, Franco M, Carrieri A, Cellamare S, Serra M, Sanna E, Biggio G, Liso G: Alpidem analogues containing a GABA or glycine moiety as new anticonvulsant agents. Eur J Pharm Sci. 2003 Mar;18(3-4):231-40.

Alpidem analogues containing a GABA (1-3) or glycine (4-6) moiety were synthesized and their interaction with the GABA/benzodiazepine receptor complex at central (CBR) and peripheral (PBR) level was evaluated.
However, compound 4 failed to interact with strychnine-sensitive Gly-binding sites.
1(0,0,0,1) Details