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LEK-8841

LEK-8841
Clinical data
Other namesLEK8841; 2-Bromo-LEK-8842; N-Methyl-N-(2-propynyl)-2-bromolysergamide; 9,10-Didehydro-N-methyl-N-(2-propynyl)-2-bromo-6-methylergoline-8β-carboxamide
Drug classMonoamine receptor modulator; Antipsychotic
ATC code
  • None
Identifiers
  • (6aR,9R)-5-bromo-N,7-dimethyl-N-prop-2-ynyl-6,6a,8,9-tetrahydro-4H-indolo[4,3-fg]quinoline-9-carboxamide
PubChem CID
ChemSpider
Chemical and physical data
FormulaC20H20BrN3O
Molar mass398.304 g·mol−1
3D model (JSmol)
  • CN1C[C@@H](C=C2[C@H]1CC3=C(NC4=CC=CC2=C34)Br)C(=O)N(C)CC#C
  • InChI=1S/C20H20BrN3O/c1-4-8-23(2)20(25)12-9-14-13-6-5-7-16-18(13)15(19(21)22-16)10-17(14)24(3)11-12/h1,5-7,9,12,17,22H,8,10-11H2,2-3H3/t12-,17-/m1/s1
  • Key:RUQRANSTJDHVEB-SJKOYZFVSA-N

LEK-8841, also known as N-methyl-N-(2-propynyl)-2-bromolysergamide or as 2-bromo-LEK-8842, is a monoamine receptor modulator of the lysergamide family related to 2-bromo-LSD.[1][2] It is the 2-bromo derivative of LEK-8842.[1][2]

The drug shows affinity for serotonin 5-HT2 and α1-adrenergic receptors (Ki = 16.3 nM at 5-HT2) and acts as a silent antagonist of these receptors (A2 = 11.7 nM and 355 nM, respectively), with activity described as qualitatively similar to that of ketanserin but with greater selectivity for serotonin 5-HT2 receptors over α1-adrenergic receptors.[1][2] However, LEK-8841 was also subsequently found to interact with the dopamine D1 and D2 receptors (Ki = 360 nM and 11.3 nM, respectively).[2] The drug inhibits apomorphine-induced hyperlocomotion and climbing behavior, induces catalepsy, inhibits the 5-hydroxytryptophan (5-HTP)-induced head twitch response, and produces hypotension in rodents.[2]

LEK-8841 was first described in the scientific literature by 1992.[1][2] It was developed by the Slovenian pharmaceutical company LEK Pharmaceuticals.[1][2] The drug has been suggested as a potential clinically effective antipsychotic for medical use.[2] Based on ratio of dopamine D2 receptor antagonism to serotonin 5-HT2 receptor antagonism, it is said to appear more like a typical than atypical antipsychotic.[2]

See also

References

  1. ^ a b c d e Krisch I, Budihna MV, Rucman R (1992). "Structure-activity study of some newly synthesized ergoline derivatives on 5-HT2 receptors and alpha-adrenoceptors in rabbit isolated aorta". Pharmacology. 45 (4): 195–208. doi:10.1159/000138998. PMID 1332086.
  2. ^ a b c d e f g h i Krisch I, Bole-Vunduk B, Pepelnak M, Lavric B, Ocvirk A, Budihna MV, et al. (October 1994). "Pharmacological studies with two new ergoline derivatives, the potential antipsychotics LEK-8829 and LEK-8841". The Journal of Pharmacology and Experimental Therapeutics. 271 (1): 343–352. doi:10.1016/S0022-3565(25)22794-X. PMID 7965734.

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