Mesulergine

Mesulergine (INNTooltip International Nonproprietary Name) (developmental code name CU-32085) is a drug of the ergoline group which was never marketed.^[1][2]

Mesulergine

Clinical data
Other names	CU-32085
Identifiers
IUPAC name N'-(1,6-dimethylergolin-8α-yl)-N,N-dimethylsulfamide
CAS Number	64795-35-3 N
PubChem CID	68848
IUPHAR/BPS	206 [3H]mesulergine: 232
ChemSpider	62081 Y
UNII	SML95FK06I
ChEBI	CHEBI:73378 N
ChEMBL	ChEMBL462903 N
CompTox Dashboard (EPA)	DTXSID3046324
Chemical and physical data
Formula	C18H26N4O2S
Molar mass	362.49 g·mol−1
3D model (JSmol)	Interactive image
SMILES O=S(=O)(N(C)C)N[C@H]2C[C@@H]3c4cccc1c4c(cn1C)C[C@H]3N(C2)C
InChI InChI=1S/C18H26N4O2S/c1-20(2)25(23,24)19-13-9-15-14-6-5-7-16-18(14)12(10-21(16)3)8-17(15)22(4)11-13/h5-7,10,13,15,17,19H,8-9,11H2,1-4H3/t13-,15+,17+/m0/s1 Y Key:JLVHTNZNKOSCNB-YSVLISHTSA-N Y
NY (what is this?)  (verify)

Pharmacology

Pharmacodynamics

Mesulergine activities

Target	Affinity (Ki, nM)	Species
5-HT1A	195–398	Human
5-HT1B	631–1,288	Human
5-HT1D	1,700–>10,000	Human
5-HT1E	ND	ND
5-HT1F	>10,000	Human
5-HT2A	19.5–151	Human
5-HT2B	1.44–3.62	Human
5-HT2C	1.12–48.5	Human
5-HT3	>10,000	Rat
5-HT4	ND	ND
5-HT5A	1,000	Rat
5-HT5B	1,000	Rat
5-HT6	776–3,800	Human
5-HT7	7.9–31.6	Human
D2	8–12	Rat
Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. Refs: [3][4][5][6]

Mesulergine acts on serotonin and dopamine receptors.^[7][8][9] Specifically, it is an agonist of dopamine D₂-like receptors and serotonin 5-HT₆ receptors and an antagonist of serotonin 5-HT_2A, 5-HT_2B, 5-HT_2C, and 5-HT₇ receptors.^{[9][additional citation(s) needed]} It also has affinity for the 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT_1F, and 5-HT_5A receptors.^[10][9]

Research

Mesulergine had entered clinical trials for the treatment of Parkinson's disease; however, further development was halted due to adverse histological abnormalities in rats.^[11] It was also investigated for the treatment of hyperprolactinemia (high prolactin levels).^[12]

See also

• Disulergine
• Etisulergine
• Quinagolide