Identification

Generic Name
LI-301
DrugBank Accession Number
DB05509
Background

LI 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.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in premature ejaculation.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

LI 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 action

LI 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.

TargetActionsOrganism
UMu-type opioid receptorNot AvailableHumans
U5-hydroxytryptamine receptor 1ANot AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Not Available
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
Not Available
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
Not Available
PubChem Substance
347910180

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

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Kind
Protein
Organism
Humans
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...
Gene Name
OPRM1
Uniprot ID
P35372
Uniprot Name
Mu-type opioid receptor
Molecular Weight
44778.855 Da
Kind
Protein
Organism
Humans
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...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da

Drug created at November 18, 2007 18:25 / Updated at June 12, 2020 16:52