Chemistry:Delergotrile

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Delergotrile (INN; 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]

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

  • Substituted ergoline

References

  1. ↑ 1.0 1.1 1.2 1.3 The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014. ISBN 978-1-4757-2085-3. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA353. Retrieved 6 May 2026. 
  2. ↑ 2.0 2.1 "Selectivity of some ergot derivatives for 5-HT1 and 5-HT2 receptors of rat cerebral cortex". General Pharmacology 17 (1): 57–62. 1986. doi:10.1016/0306-3623(86)90011-x. PMID 3949149. 
  3. ↑ 3.0 3.1 3.2 "Central monoamine synapses as sites of action for ergot drugs". Advances in Biochemical Psychopharmacology 23: 41–62. 1980. PMID 6104914. 
  4. ↑ "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. August 1983. doi:10.1016/0014-2999(83)90159-0. PMID 6311586. 
  5. ↑ 5.0 5.1 5.2 "Neurochemical effects of some ergot derivatives: a basis for their antiparkinson actions". Journal of Neural Transmission 51 (1–2): 39–59. 1981. doi:10.1007/BF01664004. PMID 6267192. 
  6. ↑ 6.0 6.1 "Neurochemical and neuropharmacological investigations with four ergot derivatives: bromocriptine, dihydroergotoxine, CF 25-397 and CM 29-712". Pharmacology 16 Suppl 1: 156–173. 1978. doi:10.1159/000136817. PMID 565520. 
  7. ↑ "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. January 1984. doi:10.1016/0014-2999(84)90525-9. PMID 6321208. 
  8. ↑ 8.0 8.1 "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. March 1978. PMID 565235. 



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