Masupirdine

Last updated

Masupirdine
Masupirdine.svg
Identifiers
  • 1-(2-bromophenyl)sulfonyl-5-methoxy-3-[(4-methylpiperazin-1-yl)methyl]indole
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C21H24BrN3O3S
Molar mass 478.41 g·mol−1
3D model (JSmol)
  • CN1CCN(CC1)CC2=CN(C3=C2C=C(C=C3)OC)S(=O)(=O)C4=CC=CC=C4Br
  • InChI=1S/C21H24BrN3O3S/c1-23-9-11-24(12-10-23)14-16-15-25(20-8-7-17(28-2)13-18(16)20)29(26,27)21-6-4-3-5-19(21)22/h3-8,13,15H,9-12,14H2,1-2H3
  • Key:GWCYPEHWIZXYFZ-UHFFFAOYSA-N

Masupirdine is an investigational new drug that is being evaluated for the treatment of agitation in Alzheimer's dementia. [1] It is a selective 5-HT6 receptor antagonist. [2]

Related Research Articles

Conatumumab is a monoclonal antibody developed for the treatment of cancer. It is a fully human monoclonal agonist antibody directed against the extracellular domain of human TRAIL receptor 2 with potential antineoplastic activity. Conatumumab mimics the activity of native TRAIL, binding to and activating TR-2, thereby activating caspase cascades and inducing tumor cell apoptosis. TR-2 is expressed by a variety of solid tumors and cancers of hematopoietic origin.

<span class="mw-page-title-main">Fedotozine</span> Chemical compound

Fedotozine is an opioid drug which acts as a peripherally specific selective κ1-opioid receptor agonist with preference for the κ1A subtype. It was under investigation for the treatment of gastrointestinal conditions like irritable bowel syndrome and functional dyspepsia and made it to phase III clinical trials, but ultimately development was discontinued and it was never marketed.

TGBA01AD (also known as FKB01MD) is a serotonin reuptake inhibitor, 5-HT1A and 5-HT1D receptor agonist, and 5-HT2 receptor antagonist which is under development by Fabre-Kramer for the treatment of major depressive disorder. It has been in phase II clinical trials since 2009, and as of January 2016, remains in this phase of development.

<span class="mw-page-title-main">Donitriptan</span> Chemical compound

Donitriptan (INN) is a triptan drug which was investigated as an antimigraine agent but ultimately was never marketed. It acts as a high-affinity, high-efficacy/near-full agonist of the 5-HT1B and 5-HT1D receptors, and is among the most potent of the triptan series of drugs. Donitriptan was being developed in France by bioMérieux-Pierre Fabre and made it to phase II clinical trials in Europe before development was discontinued.

<span class="mw-page-title-main">Selurampanel</span> Chemical compound

Selurampanel is a drug closely related to the quinoxalinedione series which acts as a competitive antagonist of the AMPA and kainate receptors and, as of 2015, is being investigated in clinical trials by Novartis for the treatment of epilepsy. It has also been studied in the acute treatment of migraine, and was found to produce some pain relief, but with a relatively high rate of side effects.

<span class="mw-page-title-main">Irampanel</span> Chemical compound

Irampanel is a drug which acts as a dual noncompetitive antagonist of the AMPA receptor and neuronal voltage-gated sodium channel blocker. It was under development by Boehringer Ingelheim for the treatment of acute stroke/cerebral ischemia but never completed clinical trials for this indication. Irampanel was also trialed, originally, for the treatment of epilepsy and pain, but these indications, too, were abandoned, and the drug was ultimately never marketed.

<span class="mw-page-title-main">Seltorexant</span> Experimental anti-insomnia drug

Seltorexant, also known by its developmental code names MIN-202 and JNJ-42847922, is an orexin antagonist medication which is under development for the treatment of depression and insomnia. It is a selective antagonist of the orexin OX2 receptor (2-SORA). The medication is taken by mouth.

<span class="mw-page-title-main">BTRX-246040</span> Nociceptin receptor antagonist

BTRX-246040, also known as LY-2940094, is a potent and selective nociceptin receptor antagonist which is under development by BlackThorn Therapeutics and Eli Lilly for the treatment of major depressive disorder (MDD). It has demonstrated proof-of-concept clinical efficacy for depression. As of 2017, it is in phase II clinical trials for the treatment of MDD. It was also under investigation for the treatment of alcoholism, and similarly reached phase II clinical studies for this indication, but development was discontinued.

<span class="mw-page-title-main">MIN-117</span> Chemical compound

MIN-117 is an investigational antidepressant which is under development by Minerva Neurosciences for the clinical treatment of major depressive disorder (MDD). It is described as a 5-HT1A and 5-HT2A receptor antagonist and inhibitor of serotonin and dopamine reuptake, and is also reported to possess affinity for the α1A- and α1B-adrenergic receptors. As of May 2015, MIN-117 is in phase II clinical trials for MDD. In December 2019, Minerva announced that MIN-117 was no longer in clinical development for MDD after disappointing results in a phase IIb trial.

Roluperidone Chemical compound

Roluperidone (former developmental code names MIN-101, CYR-101, MT-210) is a 5-HT2A and σ2 receptor antagonist under development by Minerva Neurosciences for the treatment of schizophrenia. One of its metabolites also has some affinity for the H1 receptor. Pre-clinical findings provide evidence of the effect of roluperidone on brain-derived neurotrophic factor ("BDNF"), which has been associated with neurogenesis, neuroplasticity, neuroprotection, synapse regulation, learning and memory.

<span class="mw-page-title-main">Erteberel</span> Chemical compound

Erteberel is a synthetic, nonsteroidal estrogen which acts as a selective ERβ agonist and was under development by Eli Lilly for the treatment of schizophrenia. It was specifically under investigation for the treatment of negative symptoms and cognitive impairment associated with the condition. It managed to reach phase II clinical trials for this indication in the United States in 2015. As of 2021 development has been discontinued. Erteberel was also under investigation for the treatment of benign prostatic hyperplasia and reached phase II clinical studies for this use but failed to improve symptoms in men with the condition and development for this indication was discontinued. The drug has also been proposed as a potential novel treatment for glioblastoma.

<span class="mw-page-title-main">JNJ-39393406</span> Chemical compound

JNJ-39393406 is an experimental medication which is under development by Janssen Pharmaceutica, a division of Johnson & Johnson, for the treatment of depressive disorders and smoking withdrawal. It acts as a selective positive allosteric modulator of the α7 nicotinic acetylcholine receptor (nAChR). It does not act on the α4β2 or α3β4 nAChRs or the serotonin 5-HT3 receptor, and does not interact with a panel of 62 other receptors and enzymes. The drug has been found to lower the agonist and nicotine threshold for activation of the α7 nAChR by 10- to 20-fold and to increase the maximum agonist response of the α7 nAChR by 17- to 20-fold.

<span class="mw-page-title-main">Zelquistinel</span> Investigational antidepressant compound

Zelquistinel is an orally active small-molecule NMDA receptor modulator which is under development for the treatment of major depressive disorder (MDD) by Gate Neurosciences, and previously by Allergan.

<span class="mw-page-title-main">Ralmitaront</span> Investigational antipsychotic drug

Ralmitaront is an investigational antipsychotic drug which is undergoing a clinical trial for the treatment of negative symptoms in schizophrenia and schizoaffective disorder. Another clinical trial targeting acute psychotic symptoms of schizophrenia has been terminated due to lack of efficacy. It is a partial agonist of the TAAR1. The medication is being developed by the pharmaceutical company Hoffmann-La Roche. Ralmitaront had completed phase 1 clinical trials.

<span class="mw-page-title-main">Elinzanetant</span> Chemical compound

Elinzanetant (developmental code names BAY-3427080GSK-1144814, NT-814) is an orally active small-molecule neurokinin/tachykinin NK1 receptor and NK3 receptor antagonist which is under development by Bayer, GlaxoSmithKline, and NeRRe Therapeutics for the treatment of hot flashes and "sex hormone disorders". It has been found to relieve hot flashes in postmenopausal women and to dose-dependently suppress luteinizing hormone, estradiol, and progesterone levels in premenopausal women. As of August 2021, elinzanetant is in phase 2 clinical trials for hot flashes and "sex hormone disorders". It was also under development for the treatment of schizophrenia and opioid-related disorders, but development was discontinued for these uses.

<span class="mw-page-title-main">Hypidone</span> Investigational antidepressant drug

Hypidone (developmental code name YL-0919) is an investigational serotonergic antidepressant which is under development for the treatment of major depressive disorder. It acts as a serotonin reuptake inhibitor, 5-HT1A receptor partial agonist, and 5-HT6 receptor full agonist. It is used as the hydrochloride salt. As of January 2021, hypidone is in phase 2 clinical trials for major depressive disorder.

<span class="mw-page-title-main">Posovolone</span> Chemical compound

Posovolone is a synthetic neurosteroid which was under development as a sedative/hypnotic medication for the treatment of insomnia. It is orally active and acts as a GABAA receptor positive allosteric modulator. In animals, posovolone shows anticonvulsant, anxiolytic-like, ataxic, and sleep-promoting effects and appeared to produce effects similar to those of pregnanolone. Development of the agent was started by 1999 and appears to have been discontinued by 2007. In 2021, an INNTooltip International Nonproprietary Name was registered for posovolone with the descriptor of "antidepressant". Posovolone was originally developed by Purdue Pharma.

<span class="mw-page-title-main">Dalzanemdor</span> Chemical compound

Dalzanemdor is experimental drug being investigated for the treatment of neurological disorders and cognitive impairment. It acts as a positive allosteric modulator of the NMDA receptor, whose activity is essential for learning, memory, and cognition. Dalzanemdor is an analogue of the neurosteroid 24S-hydroxycholesterol.

References

  1. "Masupirdine - Suven Life Sciences". AdisInsight. Springer Nature Switzerland AG.
  2. Nirogi R, Jayarajan P, Shinde A, Mohammed AR, Grandhi VR, Benade V, et al. (February 2023). "Progress in Investigational Agents Targeting Serotonin-6 Receptors for the Treatment of Brain Disorders". Biomolecules. 13 (2): 309. doi: 10.3390/biom13020309 . PMC   9953539 . PMID   36830678.