Adrogolide

Pharmaceutical compound From Wikipedia, the free encyclopedia

Adrogolide (INNTooltip International Nonproprietary Name; developmental code names A-93431, ABT-431, and DAS-431), also known as adrogolide hydrochloride (USANTooltip United States Adopted Name) in the case of the hydrochloride salt, is a dopamine D1-like receptor agonist which was under development for the treatment of Parkinson's disease, cognition disorders, and cocaine-related disorders but was never marketed.[2][3][4][1][5]

Other namesA-93431; ABT-431; ABT431; DAS-431; DAS431
Routes of
administrationParenteral (e.g., intravenous, inhalation)[1]
Drug classDopamine D1-like receptor agonist
ATC code
  • None
Quick facts Clinical data, Other names ...
Adrogolide
Clinical data
Other namesA-93431; ABT-431; ABT431; DAS-431; DAS431
Routes of
administration		Parenteral (e.g., intravenous, inhalation)[1]
Drug classDopamine D1-like receptor agonist
ATC code
  • None
Pharmacokinetic data
BioavailabilityOral: ≤4%[1]
Sublingual: 10–13%[1]
Inhalational: 82–107%[1]
MetabolismDeacetylation[1]
MetabolitesA-86929[1]
Elimination half-life3–4 hours[1]
Identifiers
  • [(1S,10R)-4-acetyloxy-15-propyl-14-thia-11-azatetracyclo[8.7.0.02,7.013,17]heptadeca-2,4,6,13(17),15-pentaen-5-yl] acetate
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC22H25NO4S
Molar mass399.51 g·mol−1
3D model (JSmol)
  • CCCC1=CC2=C(S1)CN[C@H]3[C@H]2C4=CC(=C(C=C4CC3)OC(=O)C)OC(=O)C
  • InChI=1S/C22H25NO4S/c1-4-5-15-9-17-21(28-15)11-23-18-7-6-14-8-19(26-12(2)24)20(27-13(3)25)10-16(14)22(17)18/h8-10,18,22-23H,4-7,11H2,1-3H3/t18-,22+/m1/s1
  • Key:KTEBZVJGMARTOQ-GCJKJVERSA-N
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It is a chemically stable and rapidly converted diacetate ester prodrug of the highly selective dopamine D1 and D5 receptor full agonist A-86929.[1] The effects of adrogolide and A-86929 in animals and humans have been studied.[1][5] Side effects of adrogolide in humans included injection site reactions, asthenia, headache, nausea, vomiting, postural hypotension, vasodilation, and dizziness.[1]

Adrogolide was under development by Abbott Laboratories and DrugAbuse Sciences.[2][3][4] It reached phase 2 clinical trials for Parkinson's disease prior to the discontinuation of its development in 2001.[2][3][4] The drug is said to have been the first extensively characterized dopamine D1 receptor full agonist.[1]

See also

References

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