6-Methyl Pergolide - CAS 57202-76-3
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
6-Methyl Pergolide
Catalog Number:
57202-76-3
Synonyms:
(8β)-6-Methyl-8-[(methylthio)methyl]ergoline;LY062;LY116467;(6aR,9R,10aR)-7-methyl-9-(methylsulfanylmethyl)-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline;LY-116467;6-Methyl-8-((methylthio)methyl)ergoline (8beta)
CAS Number:
57202-76-3
Description:
6-Methyl Pergolide is a dopamine agonist. It is also a potent antagonist of 5-HT2A and 5-HT2B receptors on porcine cardiac valves. It increases serum corticosterone concentration in rats at a dose of 3 mg/kg. It also activates brain dopaminergic receptors and lowers cranial DOPAC levels in rats.
Molecular Weight:
286.43
Molecular Formula:
C17H22N2S
Quantity:
Grams to Kilograms
Quality Standard:
In-house standard
COA:
Inquire
MSDS:
Inquire
Canonical SMILES:
CN1CC(CC2C1CC3=CNC4=CC=CC2=C34)CSC
InChI:
InChI=1S/C17H22N2S/c1-19-9-11(10-20-2)6-14-13-4-3-5-15-17(13)12(8-18-15)7-16(14)19/h3-5,8,11,14,16,18H,6-7,9-10H2,1-2H3/t11-,14-,16-/m1/s1
InChIKey:
HEZLHSNBFOCKCQ-DJSGYFEHSA-N
Targets:
Dopamine Receptor
Chemical Structure
CAS 57202-76-3 6-Methyl Pergolide

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Reference Reading


1.Effects of synthetic ergot derivatives on the two identifiable giant neurons, sensitive to dopamine, of Achatina fulica Ferussac.
Ku BS, Takeuchi H. Comp Biochem Physiol C. 1983;76(2):291-6.
On the two dopamine (DA)-sensitive giant neurones, PON (periodically oscillating neuron, excited by DA) and TAN (tonically autoactive neuron, inhibited by DA), of an African giant snail (Achatina fulica Férussac), effects of synthetic ergot derivatives, including lisuride and pergolide, which are considered to be dopamine agonists, were examined. Of the substances examined, three of the ergot derivatives related to pergolide, D-8,9-didehydro-6-propylergoline-8-methanol (LY149174), D-6-methyl-8 beta-(2-(methylsulfinyl)ethyl)ergoline (LY116470) and D-2-chloro-6-methyl-8 beta-(2-(methylsulfinyl)ethyl)ergoline (LY127817), showed excitatory effects on PON, while pergolide (D-8 beta-( (methylthio)methyl)-6-propylergoline, LY127809) and lisuride (N-D-6-methyl-8-isoergolenyl-N',N'-diethylcarbamide) had no effect. On the other hand, only D-6-methyl-8 beta-(2-(methylsulfinyl)ethyl)ergoline (LY116470) had any excitatory effects on TAN.
2.Therapeutic effects of dopamine D1/D2 receptor agonists on detrusor hyperreflexia in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned parkinsonian cynomolgus monkeys.
Yoshimura N1, Mizuta E, Yoshida O, Kuno S. J Pharmacol Exp Ther. 1998 Jul;286(1):228-33.
The effects of dopamine receptor agonists on urinary bladder function were evaluated in normal and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned parkinsonian cynomolgus monkeys to investigate the therapeutic efficacy in the treatment of urinary symptoms in Parkinson's disease. Under ketamine anesthesia, cystometrograms exhibited significant reduction in the volume threshold for the micturition reflex in MPTP-lesioned parkinsonian monkeys when compared with those of normal monkeys. The selective dopamine D2 receptor agonist bromocriptine significantly reduced the bladder volume threshold for the micturition reflex by 25 to 30% in both normal and MPTP-lesioned animals. The nonselective D1/D2 receptor agonist pergolide significantly reduced the bladder volume threshold by 22% in normal monkeys, but increased the volume threshold by 50% in MPTP-lesioned parkinsonian monkeys. Another D1/D2 agonist (5R,8R,10R)-6-methyl-8-(1,2,4-triazol-1-ylmethyl) ergoline maleate (BAM-1110) also increased the bladder volume threshold (by 80%) in parkinsonian monkeys without significant effects on the micturition reflex in normal monkeys.
3.Elevation of serum corticosterone in rats by dopamine agonists related in structure to pergolide.
Fuller RW, Snoddy HD, Mason NR, Clemens JA, Bemis KG. Neuroendocrinology. 1983;36(4):285-90.
Two chemical analogs of pergolide were examined to test further the idea that pergolide elevates serum corticosterone concentration in rats by activation of brain dopaminergic receptors. LY116467, which contains an N-methyl substituent in place of the N-n-propyl substituent in pergolide, was less potent than pergolide in lowering brain levels of 3,4-dihydroxyphenylacetic acid (Dopac), the metabolite of dopamine. LY116467 increased serum corticosterone concentration in rats at a dose of 3 mg/kg (a higher dose than is required for pergolide), and the effect was prevented by spiperone pretreatment. LY141865, which has been reported to differ from pergolide in not activating dopamine-sensitive adenylate cyclase and which was found in this study to have much less affinity for serotonin receptors than does pergolide, increased serum corticosterone in much the same manner as pergolide, only slightly higher doses being required. The effect of LY141865 was prevented by pretreatment with haloperidol but not domperidone.
4.Preclinical studies on LY237733, a potent and selective serotonergic antagonist.
Foreman MM1, Fuller RW, Nelson DL, Calligaro DO, Kurz KD, Misner JW, Garbrecht WL, Parli CJ. J Pharmacol Exp Ther. 1992 Jan;260(1):51-7.
8B-N-cyclohexyl-6-methyl-1(1-methylethyl)ergoline-8-carboxamide (LY237733) is an ergoline with potent and highly selective 5-hydroxytryptamine (5-HT) antagonist activity. The in vitro radioligand displacement studies showed that LY237733 has a preferential affinity for 5-HT1c and 5-HT2 receptors compared to other monoaminergic receptors. This characteristic is shared with other previously described ergoline 5-HT antagonists, such as LY53857 and sergolexole. In parallel ligand displacement assays, LY237733 had a similar potency to sergolexole. LY237733 was equipotent to sergolexole, but slightly less potent than LY53857 in the antagonism of 5-HT-induced elevation in blood pressure and quipazine-induced elevation in corticosterone levels, which are considered to be measures of 5-HT2 and possibly 5-HT1c antagonist activity. LY237733 failed to antagonize pergolide or 8-hydroxy-2-(di-n-propylamino)tetralin-induced elevations in serum corticosterone levels, indicating selectivity for the 5-HT1c/2 receptor, relative to 5-HT1a and D2 dopaminergic receptors.