Tracazolate

drugbox
IUPAC_name = ethyl 4-butylamino-1-ethyl-6-methylpyrazolo [4,5-e] pyridine-5-carboxylate


CAS_number = 41094-88-6
ATC_prefix =
ATC_suffix =
PubChem = 5522
DrugBank =
C=16|H=24|N=4|O=2
molecular_weight = 304.387 g/mol
bioavailability =
protein_bound =
metabolism =
elimination_half-life =
excretion =
pregnancy_AU =
pregnancy_US =
pregnancy_category=
legal_AU =
legal_CA =
legal_UK =
legal_US =
legal_status = Legal
routes_of_administration =

Tracazolate (ICI-136,753) is an anxiolytic drug which is used in scientific research. It is a pyrazolopyridine derivative, most closely related to pyrazolopyrimidine drugs such as zaleplon, and is one of a structurally diverse group of drugs known as the nonbenzodiazepines which act at the same receptor targets as benzodiazepines but have distinct chemical structures. [Patel JB, Malick JB, Salama AI, Goldberg ME. Pharmacology of pyrazolopyridines. "Pharmacology, Biochemistry and Behaviour". 1985 Oct;23(4):675-80. PMID 2866547]

Tracazolate has primarily anxiolytic and anticonvulsant effects, with sedative and muscle relaxant effects only appearing at higher doses. [Patel JB, Malick JB. Pharmacological properties of tracazolate: a new non-benzodiazepine anxiolytic agent. "European Journal of Pharmacology". 1982 Mar 12;78(3):323-33. PMID 6121711] It has a unique receptor binding profile involving allosteric modulation of several GABA_A receptor subtypes, being selective for GABA_A receptors containing α1 and β3 subunits, but exhibiting different effects depending on the third type of subunit making up the receptor complex. [Thompson SA, Wingrove PB, Connelly L, Whiting PJ, Wafford KA. Tracazolate reveals a novel type of allosteric interaction with recombinant gamma-aminobutyric acid(A) receptors. "Molecular Pharmacology". 2002 Apr;61(4):861-9. PMID 11901225]

References