Delergotrile

Delergotrile
Clinical data
Other names	CM 29-712; CM-29712; CM29-712; 6-Methylergoline-8α-acetonitrile; 6-Methyl-8α-(cyanomethyl)ergoline
Drug class	Dopamine receptor agonist; Antiparkinsonian agent
ATC code	None;
Identifiers
	IUPAC name 2-[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]acetonitrile;
CAS Number	59091-65-5;
PubChem CID	10264850;
ChemSpider	8440329;
UNII	3U2FEE7NXX;
ChEMBL	ChEMBL174095;
CompTox Dashboard (EPA)	DTXSID101024216 ;
Chemical and physical data
Formula	C17H19N3
Molar mass	265.360 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN1C[C@H](C[C@H]2[C@H]1CC3=CNC4=CC=CC2=C34)CC#N;
	InChI 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;

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]

Other namesCM 29-712; CM-29712; CM29-712; 6-Methylergoline-8α-acetonitrile; 6-Methyl-8α-(cyanomethyl)ergoline

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The drug shows high affinity for the dopamine D₂ receptor (K_i = 34 nM).^[2]^[3] In addition to dopamine receptors, delergotrile shows affinity for the serotonin 5-HT₁ receptor (K_0.5 = 2.0 nM) and for the serotonin 5-HT₂ receptor (K_i = 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