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SDZ 208-912

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SDZ 208-912
Clinical data
Other namesSDZ-208912; SDZ-HDC-912; SDZ-MAR-327; N-(2-Chloro-6-methylergoline-8α-yl)-2,2-dimethylpropanamide
Routes of
administration		Unknown[1]
Drug classDopamine D2 receptor partial agonist
ATC code
  • None
Identifiers
  • N-[(6aR,9S,10aR)-5-chloro-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]-2,2-dimethylpropanamide
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC20H26ClN3O
Molar mass359.90 g·mol−1
3D model (JSmol)
  • CC(C)(C)C(=O)N[C@H]1C[C@H]2[C@@H](CC3=C(NC4=CC=CC2=C34)Cl)N(C1)C
  • InChI=1S/C20H26ClN3O/c1-20(2,3)19(25)22-11-8-13-12-6-5-7-15-17(12)14(18(21)23-15)9-16(13)24(4)10-11/h5-7,11,13,16,23H,8-10H2,1-4H3,(H,22,25)/t11-,13+,16+/m0/s1
  • Key:QXOFQMUQMXGKGQ-NORZTCDRSA-N

SDZ 208-912 is an experimental antipsychotic of the ergoline family which was under development for the treatment of psychotic disorders but was never marketed.[1][2][3][4] Its route of administration is unknown.[1]

The drug shows high affinity for the dopamine D2 receptor, α1-adrenergic receptor, and serotonin 5-HT1A receptor, as well as somewhat lower affinity for the dopamine D1 receptor, α2-adrenergic receptor, and serotonin 5-HT2 receptor.[2] It acts as a weak partial agonist of the dopamine D2 and D3 receptors.[2][3][4][5][6] SDZ 208-912 inhibits dextroamphetamine-induced hyperlocomotion and apomorphine-induced compulsive gnawing in rodents.[2] It has a low or negligible propensity for causing catalepsy.[2][3] The drug strongly suppresses prolactin levels and produces antiparkinsonian-like effects in rodents.[2][3][4]

SDZ 208-912 was first described in the scientific literature by 1988.[2] It was under development by Novartis.[1] The drug reached phase 2 clinical trials for psychotic disorders in the United States and European Union prior to the discontinuation of its development in 1998.[1]

See also

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References

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  1. 1 2 3 4 5 "SDZ 208912". AdisInsight. 15 June 1998. Retrieved 4 June 2026.
  2. 1 2 3 4 5 6 7 Coward DM, Dixon AK, Urwyler S, Vigouret JM (November 1988). "Pharmacological properties of SDZ 208-912: a potential high potency, non-classical neuroleptic". Pharmacopsychiatry. 21 (6): 312–313. doi:10.1055/s-2007-1016990. PMID 2907635.
  3. 1 2 3 4 Coward D, Dixon K, Enz A, Shearman G, Urwyler S, White T, et al. (1989). "Partial brain dopamine D2 receptor agonists in the treatment of schizophrenia". Psychopharmacology Bulletin. 25 (3): 393–397. PMID 2576320.
  4. 1 2 3 Coward DM, Dixon AK, Urwyler S, White TG, Enz A, Karobath M, et al. (January 1990). "Partial dopamine-agonistic and atypical neuroleptic properties of the amino-ergolines SDZ 208-911 and SDZ 208-912". The Journal of Pharmacology and Experimental Therapeutics. 252 (1): 279–285. doi:10.1016/S0022-3565(25)13343-0. PMID 1967646.
  5. ↑ Tadori Y, Forbes RA, McQuade RD, Kikuchi T (November 2008). "Characterization of aripiprazole partial agonist activity at human dopamine D3 receptors". European Journal of Pharmacology. 597 (1–3): 27–33. doi:10.1016/j.ejphar.2008.09.008. PMID 18831971.
  6. ↑ Tadori Y, Forbes RA, McQuade RD, Kikuchi T (October 2011). "In vitro pharmacology of aripiprazole, its metabolite and experimental dopamine partial agonists at human dopamine D2 and D3 receptors". European Journal of Pharmacology. 668 (3): 355–365. doi:10.1016/j.ejphar.2011.07.020. PMID 21816144.
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