Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C18H26N4O2S |
Molecular Weight | 362.49 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC3=CN(C)C4=CC=CC(=C34)[C@@]1([H])C[C@@H](CN2C)NS(=O)(=O)N(C)C
InChI
InChIKey=JLVHTNZNKOSCNB-YSVLISHTSA-N
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
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL322 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7938165 |
2.0 nM [Ki] | ||
Target ID: CHEMBL324 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27061981 |
1.9 nM [Ki] | ||
8.0 nM [Ki] |
PubMed
Title | Date | PubMed |
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Treatment of Parkinson's disease with 8-alpha-amino-ergoline, CU 32-085. | 1983 Apr |
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Mechanism of action and tolerance of mesulergine. | 1984 Nov |
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The binding of serotonergic ligands to the porcine choroid plexus: characterization of a new type of serotonin recognition site. | 1984 Nov 27 |
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The effect of serotonergic agents on haloperidol-induced catalepsy. | 1990 |
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Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase. | 1993 Aug |
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Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype. | 1993 Aug 25 |
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Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor. | 1993 Mar |
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Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. | 1993 Mar |
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Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. | 1993 Nov 5 |
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Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines. | 1994 Feb |
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Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. | 1996 Jan |
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Radiolabelling of the human 5-HT2A receptor with an agonist, a partial agonist and an antagonist: effects on apparent agonist affinities. | 1996 Jan 12 |
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Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells. | 1997 Apr-May |
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Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b). | 1997 Sep |
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Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor. | 1997 Sep |
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Activating mutations of the serotonin 5-HT2C receptor. | 1997 Sep |
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[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. | 1998 Jan |
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Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. | 1998 Jul |
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The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum. | 1998 Sep |
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Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. | 2003 Sep-Nov |
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Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. | 2004 Aug |
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A 5-HT2C agonist elicits hyperactivity and oral dyskinesia with hypophagia in rabbits. | 2004 Aug |
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8-OH-DPAT as a 5-HT7 agonist: phase shifts of the circadian biological clock through increases in cAMP production. | 2004 Jan |
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Involvement of 5-hydroxytryptamine (HT)7 receptors in the 5-HT excitatory effects on the rat urinary bladder. | 2004 Nov |
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Serotonin-induced phase advances of SCN neuronal firing in vitro: a possible role for 5-HT5A receptors? | 2004 Nov |
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The role of the phosphatidyinositol-linked D1 dopamine receptor in the pharmacology of SKF83959. | 2005 Apr |
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Decreased agonist, but not antagonist, binding to the naturally occurring Thr92Lys variant of the h5-HT7(a) receptor. | 2005 Aug |
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Evidence for 5-HT2B and 5-HT7 receptor-mediated relaxation in pulmonary arteries of weaned pigs. | 2005 Jan |
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A serotonin receptor antagonist induces oocyte maturation in both frogs and mice: evidence that the same G protein-coupled receptor is responsible for maintaining meiosis arrest in both species. | 2005 Mar |
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Heterologous desensitization is evoked by both agonist and antagonist stimulation of the human 5-HT(7) serotonin receptor. | 2006 Feb 17 |
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Effects of mu-CPP and mesulergine on dietary choices in deprived rats: possible mechanisms of their action. | 2006 Jan |
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Potential vascular alpha1-adrenoceptor blocking properties of an array of 5-HT receptor ligands in the rat. | 2006 Mar 27 |
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Reanalysis of constitutively active rat and human 5-HT7(a) receptors in HEK-293F cells demonstrates lack of silent properties for reported neutral antagonists. | 2006 Oct |
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[The role of serotonergic 2C receptors in neurobiology and treatment of eating disorders]. | 2007 Jan |
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Diabetes-induced changes in 5-hydroxytryptamine modulation of vagally-induced bradycardia in rat heart. | 2007 Nov |
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Stimulation of 5-HT1A, 5-HT1B, 5-HT2A/2C, 5-HT3 and 5-HT4 receptors or 5-HT uptake inhibition: short- and long-term memory. | 2007 Nov 22 |
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Ligand sensitivity in dimeric associations of the serotonin 5HT2c receptor. | 2008 Apr |
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Serotonin activates presynaptic and postsynaptic receptors in rat globus pallidus. | 2008 Apr |
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Inverse agonist and neutral antagonist actions of antidepressants at recombinant and native 5-hydroxytryptamine2C receptors: differential modulation of cell surface expression and signal transduction. | 2008 Mar |
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Assessing the neuronal serotonergic target-based antidepressant stratagem: impact of in vivo interaction studies and knockout models. | 2008 Sep |
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Distribution and neurochemical characterization of neurons within the nucleus of the solitary tract responsive to serotonin agonist-induced hypophagia. | 2009 Jan 3 |
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The sedating antidepressant trazodone impairs sleep-dependent cortical plasticity. | 2009 Jul 1 |
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Arylbenzazepines are potent modulators for the delayed rectifier K+ channel: a potential mechanism for their neuroprotective effects. | 2009 Jun 5 |
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Upregulation of 5-HT2C receptors in hippocampus of pilocarpine-induced epileptic rats: antagonism by Bacopa monnieri. | 2009 Oct |
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Down-regulation of cerebellar 5-HT(2C) receptors in pilocarpine-induced epilepsy in rats: therapeutic role of Bacopa monnieri extract. | 2009 Sep 15 |
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Impact of RNA editing on functions of the serotonin 2C receptor in vivo. | 2010 |
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Successful drug development despite adverse preclinical findings part 2: examples. | 2010 Dec |
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Clozapine and other competitive antagonists reactivate risperidone-inactivated h5-HT7 receptors: radioligand binding and functional evidence for GPCR homodimer protomer interactions. | 2010 Dec |
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Electrophysiological effects of SKF83959 on hippocampal CA1 pyramidal neurons: potential mechanisms for the drug's neuroprotective effects. | 2010 Oct 1 |
|
Reversal of haloperidol-induced motor deficits by mianserin and mesulergine in rats. | 2011 Jan |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3517235
Initial dose were 0-5 mg mesulergine once a day. Doses were increased every 3-4 days by increments of 0-5 mg. Mesulergine the daily dose being distributed over 2-4 intakes. After the 20th day of treatment the daily dose was increased every 3-4 days by increments of 1- 0 mg, until a satisfactory therapeutic response was obtained or until significant side-effects appeared. Maximum daily doses of mesulergine was 30 mg.
Route of Administration:
Oral
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NCI_THESAURUS |
C66884
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CHEMBL12314
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SUB08793MIG
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C83940
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C031649
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73378
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5161
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DTXSID3046324
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100000081169
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MESULERGINE
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68848
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64795-35-3
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SML95FK06I
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ACTIVE MOIETY