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Pipamperone

Pipamperone
Systematic (IUPAC) name
1'-[4-(4-fluorophenyl)-4-oxobutyl]-1,4'-bipiperidine-4'-carboxamide
Clinical data
AHFS/Drugs.com
Routes of
administration
Oral
Identifiers
CAS Registry Number  N
ATC code N05
PubChem CID:
IUPHAR/BPS
ChemSpider  Y
UNII  Y
KEGG  Y
ChEMBL  Y
Synonyms McN-JR 3345; R-3345
Chemical data
Formula C21H30FN3O2
Molecular mass 375.480 g/mol
 N   

Pipamperone (INN, USAN, BAN), also known as carpiperone and floropipamide or fluoropipamide, and as floropipamide hydrochloride (JAN), is a typical antipsychotic of the butyrophenone family used in the treatment of schizophrenia.[1][2] It is or has been marketed under brand names including Dipiperon, Dipiperal, Piperonil, Piperonyl, and Propitan.[2] Pipamperone was discovered at Janssen Pharmaceutica in 1961, and entered clinical trials in the United States in 1963.[3]

Contents

  • Pharmacology 1
  • Antidepressant effects 2
  • See also 3
  • References 4

Pharmacology

Pipamperon neuraxpharm, 40mg

Pipamperone acts as an antagonist of the 5-HT2A,[4] 5-HT2B,[5] 5-HT2C[6] D2,[4] D3,[7] D4,[4][8] α1-adrenergic,[7] and α2-adrenergic receptors.[7] It shows much higher affinity for the 5-HT2A and D4 receptors over the D2 receptor (15-fold in the case of the D4 receptor, and even higher in the case of the 5-HT2A receptor),[4][7][9] being regarded as "highly selective" for the former two sites at low doses.[9][10] Pipamperone has low and likely insignificant affinity for the H1 and mACh receptors, as well as for other serotonin and dopamine receptors.[7]

Pipamperone is considered to have been a forerunner to the atypical antipsychotics, if not an atypical antipsychotic itself, due to its prominent serotonin antagonism.[11][12][13]

Antidepressant effects

Low-dose pipamperone (5 mg twice daily) has been found to accelerate and enhance the antidepressant effect of citalopram (40 mg once daily), in a combination (citalopram/pipamperone) referred to as PipCit (code name PNB-01).[9][14]

See also

References

  1. ^ Dr. Ian Morton; I.K. Morton; Judith M. Hall (31 October 1999). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 222–.  
  2. ^ a b J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 985–.  
  3. ^ David Healy (1 July 2009). The Creation of Psychopharmacology. Harvard University Press. pp. 251–.  
  4. ^ a b c d Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE (1996). "Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding". Psychopharmacology (Berl.) 124 (1-2): 57–73.  
  5. ^ Wainscott DB, Lucaites VL, Kursar JD, Baez M, Nelson DL (1996). "Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences". J. Pharmacol. Exp. Ther. 276 (2): 720–7.  
  6. ^ Prinssen EP, Koek W, Kleven MS (2000). "The effects of antipsychotics with 5-HT(2C) receptor affinity in behavioral assays selective for 5-HT(2C) receptor antagonist properties of compounds". Eur. J. Pharmacol. 388 (1): 57–67.  
  7. ^ a b c d e Bart A. Ellenbroek; Alexander R. Cools (6 December 2012). Atypical Antipsychotics. Birkhäuser. pp. 62–.  
  8. ^ Van Craenenbroeck K, Gellynck E, Lintermans B, Leysen JE, Van Tol HH, Haegeman G, Vanhoenacker P (2006). "Influence of the antipsychotic drug pipamperone on the expression of the dopamine D4 receptor". Life Sci. 80 (1): 74–81.  
  9. ^ a b c Wade AG, Crawford GM, Nemeroff CB, Schatzberg AF, Schlaepfer T, McConnachie A, Haazen L, Buntinx E (2011). "Citalopram plus low-dose pipamperone versus citalopram plus placebo in patients with major depressive disorder: an 8-week, double-blind, randomized study on magnitude and timing of clinical response". Psychol Med 41 (10): 2089–97.  
  10. ^ Michael S. Lidow (22 June 2000). Neurotransmitter Receptors in Actions of Antipsychotic Medications. CRC Press. pp. 88–.  
  11. ^ Awouters FH, Lewi PJ (2007). "Forty years of antipsychotic Drug research--from haloperidol to paliperidone--with Dr. Paul Janssen". Arzneimittelforschung 57 (10): 625–32.  
  12. ^ Vanden Bussche G, Gelders YG, Heylen SL (1990). "[Development of new antipsychotic drugs]". Acta Psiquiatr Psicol Am Lat (in Spanish; Castilian) 36 (1-2): 13–25.  
  13. ^ Niemegeers CJ, Awouters F, Janssen PA (1990). "[Serotonin antagonism involved in the antipsychotic effect. Confirmation with ritanserine and risperidone]". Encephale (in French) 16 (2): 147–51.  
  14. ^ Kirk R (2010). "Clinical trials in CNS--SMi's eighth annual conference". IDrugs 13 (2): 66–9.  
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