Pipequaline (
INN) (developmental code name PK-8165) is an
anxiolyticdrug that was never marketed.[1] It possesses a novel
chemical structure that is not closely related to other drugs of this type. The drug has a similar pharmacological profile to the
benzodiazepine family of drugs, but with mainly anxiolytic properties and very little
sedative,
amnestic or
anticonvulsant effects, and so is classified as a
nonbenzodiazepine anxiolytic.[2][3][4]
Pipequaline acts as a non-selective
GABAA receptor
partial agonist.[5][6][7] While its profile of anxiolytic effects without sedation would appear to have potential medical applications, pipequaline has never been developed for medical use and is currently only used in scientific research.
^von Frenckell R, Ansseau M, Bonnet D (January 1986). "Evaluation of the sedative properties of PK 8165 (pipequaline), a benzodiazepine partial agonist, in normal subjects". International Clinical Psychopharmacology. 1 (1): 24–35.
doi:
10.1097/00004850-198601000-00004.
hdl:2268/259698.
PMID3559150.
^Willer JC, Von Frenkell R, Bonnet D, Le Fur G (March 1986). "The ability of PK 8165, a quinoline derivative, to reduce responses to a stressful situation in a double-blind study in man". Neuropharmacology. 25 (3): 275–81.
doi:
10.1016/0028-3908(86)90252-2.
PMID3703176.
S2CID42473917.
^Eves FF, Curran HV, Shine P, Lader MH (1988). "The effects on memory of pipequaline, alone or in combination with diazepam". Psychopharmacology. 95 (3): 386–9.
doi:
10.1007/BF00181953.
PMID3137626.
S2CID20460757.
^Mizoule J, Rataud J, Uzan A, Mazadier M, Daniel M, Gauthier A, et al. (October 1984). "Pharmacological evidence that PK 8165 behaves as a partial agonist of brain type benzodiazepine receptors". Archives Internationales de Pharmacodynamie et de Therapie. 271 (2): 189–97.
PMID6095778.
^Benavides J, Malgouris C, Flamier A, Tur C, Quarteronet D, Begassat F, et al. (October 1984). "Biochemical evidence that 2-phenyl-4[(4-piperidinyl) ethyl]quinoline, a quinoline derivative with pure anticonflict properties, is a partial agonist of benzodiazepine receptors". Neuropharmacology. 23 (10): 1129–36.
doi:
10.1016/0028-3908(84)90229-6.
PMID6097832.
S2CID36082385.
^Debonnel G, de Montigny C (September 1987). "Pipequaline acts as a partial agonist of benzodiazepine receptors: an electrophysiological study in the hippocampus of the rat". Neuropharmacology. 26 (9): 1337–42.
doi:
10.1016/0028-3908(87)90096-7.
PMID2823163.
S2CID38530030.