Berupipam Explained

Class:Dopamine D1 receptor antagonist
Cas Number:150490-85-0
Pubchem:66002
Chemspiderid:59394
Unii:420895MAOC
Chembl:2106005
Synonyms:NNC 22-0010; NNC-22-0010; NNC220010; NNC2210; NNC-2210
Iupac Name:(5S)-5-(5-bromo-2,3-dihydro-1-benzofuran-7-yl)-8-chloro-3-methyl-1,2,4,5-tetrahydro-3-benzazepin-7-ol
C:19
H:19
Br:1
Cl:1
N:1
O:2
Smiles:CN1CCC2=CC(=C(C=C2[C@H](C1)C3=CC(=CC4=C3OCC4)Br)O)Cl
Stdinchi: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
Stdinchikey:DIKLCFJDIZFAOM-INIZCTEOSA-N

Berupipam (; 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.

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.

See also

Notes and References

  1. Web site: BERUPIPAM . Inxight Drugs . 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 . Dopamine D1 receptor ligands: where are we now and where are we going . Med Res Rev . 29 . 2 . 272–294 . March 2009 . 18642350 . 10.1002/med.20130 .
  3. Hall . Rodger . Defining new ground for the treatment of schizophrenia . Inpharma Weekly . Springer Science and Business Media LLC . 953 . 953. 1994 . 1173-8324 . 10.2165/00128413-199409530-00015 . 8–9 . 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 . Radioligands for the dopamine receptor subtypes . J Labelled Comp Radiopharm . 56 . 3–4 . 130–148 . 2013 . 24285319 . 10.1002/jlcr.3000 .
  5. Banerjee A, Prante O . Subtype-selective dopamine receptor radioligands for PET imaging: current status and recent developments . Curr Med Chem . 19 . 23 . 3957–3966 . 2012 . 22780960 . 10.2174/092986712802002518 .
  6. Foged C, Halldin C, Loc'h C, Mazière B, Karlsson P, Mazière M, Swahn CG, Farde L . 11C- and 76Br-labelled NNC 22-0010, selective dopamine D1 receptor radioligands for PET . Nucl Med Biol . 23 . 6 . 837–844 . August 1996 . 8940728 . 10.1016/0969-8051(96)00083-2 .

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