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Identification
NameLI-301
Accession NumberDB05509
TypeSmall Molecule
GroupsInvestigational
DescriptionLI 301 is an orally bio-available compound delivered in a fast melt mechanism with taste masking enabling it to be taken anytime without water. It has a novel mode of action combining both the light effect of a Selective Serotonin Reuptake Inhibitor ("SSRI")(most likely antagonistic at 5HT1a receptors) and antagonism at mu-opioid receptors. This results in a slight dulling of sensation that can be used to treat premature ejaculation without interfering with normal sexual pleasure or orgasm.
Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
CategoriesNot Available
UNIINot Available
CAS numberNot Available
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Pharmacology
IndicationInvestigated for use/treatment in premature ejaculation.
Structured Indications Not Available
PharmacodynamicsLI 301 is an orally bio-available compound delivered in a fast melt mechanism with taste masking enabling it to be taken anytime without water. LI 301 is active in the system for up to seven hours once administered, enabling patients to relax and partners to feel unpressured by time limitation. LI 301 has a novel mode of action combining both the light effect of a Selective Serotonin Reuptake Inhibitor ("SSRI") and u-opioid. This results in a slight dulling of sensation that can be used to treat premature ejaculation without interfering with normal sexual pleasure or orgasm.
Mechanism of actionLI 301 has a novel mode of action combining both the light effect of a Selective Serotonin Reuptake Inhibitor ("SSRI")(most likely antagonistic at 5HT1a receptors) and antagonism at mu-opioid receptors.
TargetKindPharmacological actionActionsOrganismUniProt ID
Mu-type opioid receptorProteinunknownNot AvailableHumanP35372 details
5-hydroxytryptamine receptor 1AProteinunknownNot AvailableHumanP08908 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External LinksNot Available
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Taxonomy
ClassificationNot classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Voltage-gated calcium channel activity
Specific Function:
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociati...
Gene Name:
OPRM1
Uniprot ID:
P35372
Molecular Weight:
44778.855 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
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Drug created on November 18, 2007 11:25 / Updated on August 17, 2016 12:24