Berupipam

Last updated
Berupipam
Berupipam.svg
Clinical data
Other namesNNC 22-0010; NNC-22-0010; NNC220010; NNC2210; NNC-2210
Drug class Dopamine D1 receptor antagonist
Identifiers
  • (5S)-5-(5-bromo-2,3-dihydro-1-benzofuran-7-yl)-8-chloro-3-methyl-1,2,4,5-tetrahydro-3-benzazepin-7-ol
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C19H19BrClNO2
Molar mass 408.72 g·mol−1
3D model (JSmol)
  • CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC(=CC4=C3OCC4)Br)O)Cl
  • InChI=1S/C19H19BrClNO2/c1-22-4-2-11-7-17(21)18(23)9-14(11)16(10-22)15-8-13(20)6-12-3-5-24-19(12)15/h6-9,16,23H,2-5,10H2,1H3/t16-/m0/s1
  • Key:DIKLCFJDIZFAOM-INIZCTEOSA-N

Berupipam (INN Tooltip International Nonproprietary Name; developmental code name NNC 22-0010) is a selective dopamine D1 receptor antagonist of the benzazepine group which was under development for the treatment of psychotic disorders but was never marketed. [1] [2] It reached phase 1 clinical trials prior to the discontinuation of its development. [1]

Berupipam and closely related dopamine D1 receptor antagonists were reported to have been generally well-tolerated in clinical trials, but side effects included restlessness, drowsiness, other central nervous system-related symptoms, and orthostatic hypotension. [3]

Berupipam, in radiolabeled form, has been studied for use in positron emission tomography (PET) imaging. [4] [5] [6] The drug was first described in the scientific literature by 1994. [3]

See also

References

  1. 1 2 "BERUPIPAM". Inxight Drugs. Retrieved 21 October 2024. Berupipam (also known as NNC 22-0010), a dopamine antagonist with a high affinity and selectivity for D1 receptor has been studied for patients with psychotic disorders. Berupipam participated in phase I clinical trials; however, further development of this drug was discontinued
  2. ↑ Zhang J, Xiong B, Zhen X, Zhang A (March 2009). "Dopamine D1 receptor ligands: where are we now and where are we going". Med Res Rev. 29 (2): 272–294. doi:10.1002/med.20130. PMID   18642350.
  3. 1 2 Hall, Rodger (1994). "Defining new ground for the treatment of schizophrenia". Inpharma Weekly. 953 (953). Springer Science and Business Media LLC: 8–9. doi:10.2165/00128413-199409530-00015. ISSN   1173-8324. D1-antagonists are an area of active research. Although no results of widespread clinical testing have yet been published. phase I clinical trials presented by Dr M Sloth-Nielson from Novo Nordisk suggest that further investigation of the 3 novel drugs NNC 01-0687, NNC 01-0756 [odapipam] and NNC 22-0010 is warranted. The drugs were generally well tolerated, with restlessness, drowsiness and other CNS-related symptoms being the main effects observed. NNC 22-0010 50mg produced a moderate orthostatic hypotension in 2 volunteers.
  4. ↑ Prante O, Maschauer S, Banerjee A (2013). "Radioligands for the dopamine receptor subtypes". J Label Compd Radiopharm. 56 (3–4): 130–148. doi:10.1002/jlcr.3000. PMID   24285319.
  5. ↑ Banerjee A, Prante O (2012). "Subtype-selective dopamine receptor radioligands for PET imaging: current status and recent developments". Curr Med Chem. 19 (23): 3957–3966. doi:10.2174/092986712802002518. PMID   22780960.
  6. ↑ Foged C, Halldin C, Loc'h C, Mazière B, Karlsson P, Mazière M, Swahn CG, Farde L (August 1996). "11C- and 76Br-labelled NNC 22-0010, selective dopamine D1 receptor radioligands for PET". Nucl Med Biol. 23 (6): 837–844. doi:10.1016/0969-8051(96)00083-2. PMID   8940728.


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