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Details

Stereochemistry ABSOLUTE
Molecular Formula C12H17NO.C4H6O4
Molecular Weight 309.3575
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PHENDIMETRAZINE SUCCINATE

SMILES

OC(=O)CCC(O)=O.C[C@H]1[C@@H](OCCN1C)C2=CC=CC=C2

InChI

InChIKey=FYHWTGPJFRUSFQ-XOZOLZJESA-N
InChI=1S/C12H17NO.C4H6O4/c1-10-12(14-9-8-13(10)2)11-6-4-3-5-7-11;5-3(6)1-2-4(7)8/h3-7,10,12H,8-9H2,1-2H3;1-2H2,(H,5,6)(H,7,8)/t10-,12+;/m0./s1

HIDE SMILES / InChI

Molecular Formula C12H17NO
Molecular Weight 191.2695
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula C4H6O4
Molecular Weight 118.088
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Phendimetrazine is an appetite suppressant that is FDA approved for the treatment of exogenous obesity. It is clinically available anorectic agent, which display minimal interactions with monoamine transporters in vitro. On the other hand, their medications is known to be psychomotor stimulants when administered in vivo as indicated by their shared properties with illicit drugs like cocaine. The following adverse reactions are described, or described in greater detail, in other sections: Primary pulmonary hypertension; Valvular heart disease; Effect on the ability to engage in potentially hazardous tasks; Withdrawal effects following prolonged high dosage administration. Use of phendimetrazine tartrate is contraindicated during or within 14 days following the administration of monoamine oxidase inhibitors because of the risk of hypertensive crisis.

CNS Activity

Originator

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
2.56 µM [EC50]
8.3 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
PHENDIMETRAZINE TARTRATE
PubMed

PubMed

TitleDatePubMed
Safety and tolerability of intranasal cocaine during phendimetrazine maintenance.
2016 Jun
Attenuation of cocaine self-administration by chronic oral phendimetrazine in rhesus monkeys.
2016 Jun 2
Abuse Potential of Oral Phendimetrazine in Cocaine-dependent Individuals: Implications for Agonist-like Replacement Therapy.
2016 May-Jun
Patents

Sample Use Guides

In Vivo Use Guide
One extended-release capsule (105 mg phendimetrazine tartrate) in the morning (30 to 60 minutes before morning meal).
Route of Administration: Oral
In Vitro Use Guide
Racemic phendimetrazine was essentially inactive at [3H]dopamine, [3H]norepinephrine, and [3H]5-HT uptake inhibition and release. The most potent effect of phendimetrazine was inhibition of [3H]norepinephrine uptake, with an IC50 of 8300 nM.
Substance Class Chemical
Created
by admin
on Tue Oct 22 19:08:57 UTC 2019
Edited
by admin
on Tue Oct 22 19:08:57 UTC 2019
Record UNII
0Q1YTA0F4B
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PHENDIMETRAZINE SUCCINATE
Common Name English
Code System Code Type Description
PUBCHEM
76960510
Created by admin on Tue Oct 22 19:08:57 UTC 2019 , Edited by admin on Tue Oct 22 19:08:57 UTC 2019
PRIMARY
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ACTIVE MOIETY