GABA Receptors

Cat. No.

A11782

CAS No.

124423-84-3

Panadiplon

Synonyms: FG 10571; PNU 78875

Panadiplon is a partial agonist of the GABA(A) receptor, specifically targeting the 5GABA(A) subtype with notable selectivity over the 1GABA(A) subtype. This compound demonstrates significant anxiolytic properties and is employed in research applications related to anxiety disorders and other neuropharmacological studies. Its selective action makes Panadiplon a valuable tool for investigating the role of GABA(A) receptor subtypes in the central nervous system.

Cat. No.

A12875

CAS No.

205701-85-5

RWJ-51204

RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

Cat. No.

A13357

CAS No.

170568-47-5

U-101017

Synonyms: PNU 101017

U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.

Cat. No.

A20152

CAS No.

194098-25-4

CP-409092

CP-409092 is a partial agonist of GABAA receptor, with anti-anxiety activity.

Cat. No.

A21397

CAS No.

225240-86-8

CP-409092 hydrochloride

Synonyms: CP409092

CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity.

Cat. No.

A66624

CAS No.

425377-76-0

TPA-023B

TPA-023B is an orally active partial agonist at the GABAA receptor α2 and α3 subtypes, with affinities of 0.73 nM and 2 nM, respectively, while acting as an antagonist at the α1 subtype with a Ki of 1.8 nM. This compound exhibits non-sedating anxiolytic-like properties, making it a valuable tool for research into anxiety disorders and GABAergic signaling. Its selective modulation of specific GABA receptor subtypes allows for nuanced studies on neuropharmacological effects.

Cat. No.

A66625

CAS No.

498-94-2

Isonipecotic acid

Isonipecotic acid is a GABAA receptor partial agonist that modulates inhibitory neurotransmission in the central nervous system. Its biological activity includes the potential to enhance GABAergic signaling, making it a valuable tool for studying anxiety, seizure disorders, and other neurophysiological processes. This compound is applicable in research focused on developing therapeutic strategies for CNS-related conditions.

Cat. No.

A66639

CAS No.

233275-76-8

MK-0343

Synonyms: MRK-409

MK-0343 is an orally bioavailable partial agonist selective for the GABA(A) receptor subtype. This compound exhibits anxiolytic properties without sedation, making it a valuable tool for neurological research. MK-0343 is utilized in studies involving anxiety disorders and the modulation of neurotransmitter systems, contributing to the understanding of therapeutic approaches for related conditions.

Cat. No.

A66652

CAS No.

286456-42-6

L-838417

L-838417 is a selective partial agonist targeting the α2, α3, and α5 subtypes of the GABAA receptor while functioning as an antagonist at the α1 subtype. With binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM, and 2183 nM for various receptor subtypes, L-838417 exhibits significant anti-anxiety effects. This reagent is valuable for research on anxiety disorders and the modulation of GABAergic neurotransmission.

Cat. No.

A66699

CAS No.

172986-25-3

Cinazepam

Cinazepam is a partial agonist of the GABAA receptor and belongs to the benzodiazepine class. It exhibits anxiolytic and sedative effects, making it a valuable tool in the study of sleep disorders and anxiety-related conditions. Research utilizing Cinazepam can provide insights into the modulation of GABAergic signaling and its implications for therapeutic applications.

Cat. No.

A66705

CAS No.

96604-21-6

Ocinaplon

Synonyms: DOV 273547

Ocinaplon is a partial agonist of the GABAA receptor, specifically functioning as a positive allosteric modulator with notable efficacy at the α1 subunit. This compound demonstrates potential anxiolytic effects, making it valuable for research in anxiety disorders and related neurological conditions. Its mechanism of action offers insight into therapeutic strategies targeting GABAergic pathways.

Cat. No.

A66706

CAS No.

133737-32-3

Pagoclone

Synonyms: (+)-RP-59037; IP-456; RP-62955

Pagoclone is a selective partial agonist of the GABA(A) receptor. It exhibits anxiolytic properties, making it relevant for research into the modulation of anxiety and panic disorders. Its unique profile allows for the investigation of GABAergic mechanisms in neurological research and pharmacological studies.

Cat. No.

A66831

CAS No.

111841-85-1

Abecarnil

Synonyms: ZK 112119

Abecarnil is a partial agonist of the benzodiazepine (BZ) receptor, functioning primarily as a positive allosteric modulator of the GABAA receptor. It exhibits significant anxiolytic and anticonvulsant properties, making it valuable in neuroscience research. Abecarnil effectively inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM, and is particularly useful in studies related to epilepsy.

Cat. No.

A66853

CAS No.

122384-14-9

L-663581

Synonyms: FG-8205

L-663581 is a partial agonist specifically targeting the GABA A receptor through the benzodiazepine receptor. This compound exhibits notable anxiolytic and sedative properties, making it valuable for research into neurological conditions and potential therapeutic applications for anxiety disorders. Its modulation of GABAergic neurotransmission provides insights into the mechanisms of action for anxiolytic agents.

Cat. No.

A66867

CAS No.

329016-45-7

CP-615003

Synonyms: NGD-913

CP-615003 is a potent partial agonist of the GABAA receptor, exhibiting subtype-selectivity with a Ki value of 1.1 μM. This compound is converted into the active metabolite CP-900725 through oxidative deamination, which also shows affinity for the GABAA receptor. Additionally, CP-615003 is a substrate of P-glycoprotein, which may restrict its central nervous system penetration. It is primarily used in research related to CNS disorders and functions of the GABAA receptor.

Cat. No.

A66972

CAS No.

188116-08-7

ELB-139

ELB-139 is a GABAA receptor partial agonist known for its anxiolytic and anticonvulsant properties. This progesterone analogue modulates GABAA receptor activity, demonstrating significant effects on neurotransmitter levels, particularly enhancing extracellular serotonin (5-HT) in the striatum and medial prefrontal cortex of rodent models. ELB-139 holds potential for research applications related to anxiety disorders and seizure disorders.