Wikipedia

Delergotrile

Delergotrile (INNTooltip International Nonproprietary Name; developmental code name CM 29-712), also known as 6-methylergoline-8α-acetonitrile, is a dopamine receptor agonist of the ergoline family described as an antiparkinsonian agent which was never marketed.[1] It is an analogue of lergotrile (LY-79907).[1]

Delergotrile
Clinical data
Other namesCM 29-712; CM-29712; CM29-712; 6-Methylergoline-8α-acetonitrile; 6-Methyl-8α-(cyanomethyl)ergoline
Drug classDopamine receptor agonist; Antiparkinsonian agent
ATC code
  • None
Identifiers
  • 2-[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]acetonitrile
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H19N3
Molar mass265.360 g·mol−1
3D model (JSmol)
  • CN1C[C@H](C[C@H]2[C@H]1CC3=CNC4=CC=CC2=C34)CC#N
  • InChI=1S/C17H19N3/c1-20-10-11(5-6-18)7-14-13-3-2-4-15-17(13)12(9-19-15)8-16(14)20/h2-4,9,11,14,16,19H,5,7-8,10H2,1H3/t11-,14+,16+/m0/s1
  • Key:LBMFWYCMCHRLBU-SGIREYDYSA-N

The drug shows high affinity for the dopamine D2 receptor (Ki = 34 nM).[2][3] In addition to dopamine receptors, delergotrile shows affinity for the serotonin 5-HT1 receptor (K0.5 = 2.0 nM) and for the serotonin 5-HT2 receptor (Ki = 57 nM),[2][3] as well as for the α1- and α2-adrenergic receptors.[4] The drug appears to be an agonist of both dopamine D1 and to a lesser extent D2 receptors.[5] Due to its dopamine receptor agonism, delergotrile produces antiparkinsonian-like effects, induces changes in locomotor activity and stereotypy, and reverses reserpine-induced akinesia in rodents.[6][5] It also produces effects consistent with weak blockade of α-adrenergic receptors in rodents.[6][3][5][7]

Delergotrile was first described in the literature by 1976.[1][8] It was developed by Sandoz.[1][8]

See also

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References

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  1. 1 2 3 4 Elks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. ISBN 978-1-4757-2085-3. Retrieved 6 May 2026.
  2. 1 2 Beart PM, McDonald D, Cincotta M, de Vries DJ, Gundlach AL (1986). "Selectivity of some ergot derivatives for 5-HT1 and 5-HT2 receptors of rat cerebral cortex". General Pharmacology. 17 (1): 57–62. doi:10.1016/0306-3623(86)90011-x. PMID 3949149.
  3. 1 2 3 Fuxe K, Ogren SO, Agnati LF, Andersson K, Hall H, Köhler C, et al. (1980). "Central monoamine synapses as sites of action for ergot drugs". Advances in Biochemical Psychopharmacology. 23: 41–62. PMID 6104914.
  4. ↑ McPherson GA, Beart PM (August 1983). "The selectivity of some ergot derivatives for alpha 1 and alpha 2-adrenoceptors of rat cerebral cortex". European Journal of Pharmacology. 91 (4): 363–369. doi:10.1016/0014-2999(83)90159-0. PMID 6311586.
  5. 1 2 3 Markstein R (1981). "Neurochemical effects of some ergot derivatives: a basis for their antiparkinson actions". Journal of Neural Transmission. 51 (1–2): 39–59. doi:10.1007/BF01664004. PMID 6267192.
  6. 1 2 Vigouret JM, Bürki HR, Jaton AL, Züger PE, Loew DM (1978). "Neurochemical and neuropharmacological investigations with four ergot derivatives: bromocriptine, dihydroergotoxine, CF 25-397 and CM 29-712". Pharmacology. 16 Suppl 1: 156–173. doi:10.1159/000136817. PMID 565520.
  7. ↑ McPherson GA (January 1984). "In vitro selectivity of lisuride and other ergot derivatives for alpha 1- and alpha 2-adrenoceptors". European Journal of Pharmacology. 97 (1–2): 151–155. doi:10.1016/0014-2999(84)90525-9. PMID 6321208.
  8. 1 2 Jaton AL, Loew DM, Vigouret JM (March 1978). "A comparison of apomorphine, bromocriptine and Sandoz CM 29-712 (6-methyl-8a-cyanomethyl-ergoline-l) in four different turning models in the rat [proceedings]". British Journal of Pharmacology. 62 (3): 395P. PMC 1668167. PMID 565235.
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