Chemistry:Berupipam
Berupipam (INN; 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
- Substituted 3-benzazepine
- List of investigational antipsychotics
- Ecopipam (SCH-39166)
- NNC 01-0687 (ADX-10061)
- Odapipam (NNC 01-0756)
- SCH-23390
References
- ↑ 1.0 1.1 "BERUPIPAM". https://drugs.ncats.io/substance/420895MAOC. "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"
- ↑ "Dopamine D1 receptor ligands: where are we now and where are we going". Med Res Rev 29 (2): 272–294. March 2009. doi:10.1002/med.20130. PMID 18642350.
- ↑ 3.0 3.1 Hall, Rodger (1994). "Defining new ground for the treatment of schizophrenia". Inpharma Weekly (Springer Science and Business Media LLC) 953 (953): 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.".
- ↑ "Radioligands for the dopamine receptor subtypes". J Label Compd Radiopharm 56 (3–4): 130–148. 2013. doi:10.1002/jlcr.3000. PMID 24285319.
- ↑ "Subtype-selective dopamine receptor radioligands for PET imaging: current status and recent developments". Curr Med Chem 19 (23): 3957–3966. 2012. doi:10.2174/092986712802002518. PMID 22780960.
- ↑ "11C- and 76Br-labelled NNC 22-0010, selective dopamine D1 receptor radioligands for PET". Nucl Med Biol 23 (6): 837–844. August 1996. doi:10.1016/0969-8051(96)00083-2. PMID 8940728.
 |  |
