benzodiazepine receptor

Sarmazenil (Ro 15-3505) is a partial inverse agonist at the benzodiazepine receptor with pro-convulsant properties and is used in the study of chronic hepatic encephalopathy (HE).

Ro 41-3290, the desethylated derivative of Ro 41-3696, is a nonbenzodiazepine partial agonist at the benzodiazepine receptor.

FG8119 is a novel benzodiazepine agonist with potential anticonvulsant and antiepileptic activity for studying neurological disorders.

CGS8216 is a benzodiazepine receptor antagonist that shows analgesic activity at high doses.CGS8216 has anxiolytic activity and may be used to study immune system disorders.

high affinity agonist of the translocator protein

Harman hydrochloride can directly induce CYP1A1 gene expression in an AhR-dependent manner and may represent a novel mechanism by which harman promotes mutagenicity, co-mutagenicity and carcinogenicity.

CGS 20625 is an orally active, specific, and potent partial agonist at the central benzodiazepine receptor with anxiolytic and anticonvulsant activity.CGS 20625 inhibits the binding of [3H]-flunitrazepam to the central benzodiazepine receptor and can be used in studies of neurological disorders such as anxiety and epilepsy.

Emapunil (XBD-173) is an anxiolytic drug which acts as a selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO.

Harmane (Loturine) is a bio-active β-Carboline and monoamine oxidase inhibitor found in coffee and tobacco smoke.

DAA-1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), acting as a potent and selective agonist at the peripheral benzodiazepine receptor.

DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA αxβ3γ2 receptor subtypes. For α1, α2, α3, and α5 receptors, their Kis were 10 nM, 13 nM, 7.5 nM, 2.2 nM, respectively.

Ru-32514 is a benzodiazepine receptor agonist that partially reverses stress-induced arousal in mice and is used in the study of neurological disorders.

Panadiplon (FG 10571) is a selective gamma-aminobutyric acid receptor agonist and partial agonist of 5GABAA, a benzodiazepine receptor, used in the treatment of anxiety disorders.Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.

Flumazenil (Ro 15-1788) antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS), thereby preventing the chloride channel opening events and inhibiting neuronal hyperpolarization. As a result, flumazenil reverses benzodiazepine-induced effects including sedation, psychomotor deficits, amnesia, and hypoventilation in a dose-dependent manner. Flumazenil is an imidazobenzodiazepine derivative, effective in reversing benzodiazepine-induced activities.

1. Pulegone ((+)-Pulegone) has cytotoxicity followed by regenerative cell proliferation is the MOA for Pulegone-induced urothelial tumors in female rats. 2. Pulegone induces a verapamil-sensitive psychostimulant effect that appears to independ on the opening of L-type calcium channels. 3. Pulegone has negative reinforcing properties and seems to possess anxiolytic-like actions unrelated to the benzodiazepine site of the γ-aminobutyric acid type A (GABAA) receptor.

4,4-dimethyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one is a benzodiazepine derivative. It is an orthosteric modulator of the GABAA receptor and selectively binds to the benzodiazepine site of the GABAA receptor. It has anxiolytic, anticonvulsant and sedative activity.

Cirsiliol is a 5-lipoxygenase (5-LOX) inhibitor and low affinity benzodiazepine receptor ligand.Cirsiliol inhibits cell proliferation and promotes apoptosis of OS cells.Cirsiliol shows antitumor activity against OS cells in an in situ xenograft tumor model and can be used to study colon cancer.

FG 7142 (LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex. FG 7142 , a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM).

S-8510 phosphate is an agonist of inverse Benzodiazepine (BDZ) receptor(Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively).

PK14105 has been evaluated biologically as a potential radioligand for positron emission tomography (PET) studies targeting peripheral benzodiazepine binding sites (PBBS) receptors. When administered to rats with unilaterally lesioned striata, PK14105 was observed to quickly cross the blood-brain barrier, displaying significant radioactivity retention in the lesioned striatum, in contrast to the unlesioned striatum or cerebellar vermis. Additionally, PK14105 has the capability to inhibit receptor ligands, calcium channel ligands, and co-transporters in all salivary glands.

Radequinil is a benzodiazepine receptor partial inverse agonist. Rade quinil binds to GABA(-) and GABA(+) ligand (Kis: 5.15 and 6.11 nM, respectively).

U-101017 is a partial benzodiazepine receptor and GABAA receptor agonist.

Imepitoin (AWD 131-138) is a novel low-affinity partial benzodiazepine receptor agonist, exhibiting potent anticonvulsant and anxiolytic properties in rodent models.

L-838417 is a GABAA receptor subtype-selective benzodiazepine site-selective ligand and GABAA receptor-positive modulator.L-838417 is a selective partial agonist of the α2, α3, and α5 subtypes and an antagonist of the α1 subtype and is used in the study of anxiety disorders.