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A 86929
a selective dopamine D1 agonists; structure given in first source
Also Known As:
2-propyl-4,5,5a,6,7,11b-hexahydro-3-thia-5-azacyclopent-1-ena(c)phenanthrene-9,10-diol; 4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1-ena(c)phenanthrene-9,10-diol; A-86929
Networked:
5
relevant articles (
2
outcomes,
2
trials/studies)
Relationship Network
Bio-Agent Context: Research Results
Organic Chemicals: 133
Sulfur Compounds: 278
Thiophenes: 257
A 86929: 5
Heterocyclic Compounds: 198
1-Ring Heterocyclic Compounds
Thiophenes: 257
A 86929: 5
Fused-Ring Heterocyclic Compounds
2-Ring Heterocyclic Compounds
Quinolines: 146
Quinolones: 2938
A 86929: 5
Related Diseases
1.
Parkinson Disease (Parkinson's Disease)
01/01/1996 - "
A-86929 and ABT-431 improved behavioral disability scores and increased locomotor activity in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned marmoset model of Parkinson's disease in a dose-dependent manner (the minimum effective dose was 0.10 mumol/kg s.c.).
"
04/01/1997 - "
This study suggests that a selective D1 receptor agonist, such as A-86929, with full intrinsic activity relative to dopamine, may be useful for the treatment of Parkinson's disease.
"
04/01/1997 - "
The selective dopamine D1 receptor agonist A-86929 maintains efficacy with repeated treatment in rodent and primate models of Parkinson's disease.
"
01/01/1996 - "
An agent such as A-86929 (or its prodrug ABT-431), which selectively stimulates the D1 receptor, may represent a novel mechanism for Parkinson's disease therapy with the potential for an improved side-effect profile and, consequently, improved patient compliance.
"
01/01/1996 - "
ABT-431: the diacetyl prodrug of A-86929, a potent and selective dopamine D1 receptor agonist: in vitro characterization and effects in animal models of Parkinson's disease.
"
2.
Dyskinesias (Dyskinesia)
02/01/1999 - "
In these L-dopa-primed animals, A-86929 effectively reversed akinesia and produced dose-dependent dyskinesias which were significantly less intense than those produced by L-dopa administration.
"
08/01/1997 - "
Acute administration of A-86929 was as efficacious in alleviating MPTP-induced parkinsonism as levodopa and LY-171555, but was less likely to reproduce the levodopa-induced dyskinesias in these animals than with either LY-171555 or subsequent challenge of levodopa.
"
08/01/1997 - "
We therefore conducted the present acute dose-response study in four 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-exposed cynomolgus monkeys primed to exhibit levodopa-induced dyskinesias to evaluate the locomotor and dyskinetic effects on challenge with four doses (from 0.03 to 1.0 mg/kg) of A-86929 ([-]-[5aR,11bS]-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-+ ++azacyclopent-1- ena[c]phenathrene-9-10-diol), a selective and full DA D1-like receptor agonist with an intermediate duration of action.
"
02/01/1999 - "
These results show a lesser liability of A-86929 and A-77636 to reproduce dyskinesia in L-dopa-primed MPTP-lesioned subjects while maintaining effective antiparkinsonian activity and producing a more naturalistic motor response.
"
02/01/1999 - "
Actions of the D1 agonists A-77636 and A-86929 on locomotion and dyskinesia in MPTP-treated L-dopa-primed common marmosets.
"
3.
MPTP Poisoning
08/01/1997 - "
Acute administration of A-86929 was as efficacious in alleviating MPTP-induced parkinsonism as levodopa and LY-171555, but was less likely to reproduce the levodopa-induced dyskinesias in these animals than with either LY-171555 or subsequent challenge of levodopa.
"
4.
Seizures (Absence Seizure)
12/19/1996 - "
Young rats (35-37 days) exhibited behavioral seizures following A-86929 and ABT-431 treatment (ED50 = 34.2 and 35.6 mumol/kg, s.c., respectively), but at doses higher than those required in mice.
"
12/19/1996 - "
Hyperactivity and behavioral seizures in rodents following treatment with the dopamine D1 receptor agonists A-86929 and ABT-431.
"
Related Drugs and Biologics
1.
Dopamine (Intropin)
2.
Dopamine D1 Receptors (Dopamine D1 Receptor)
3.
adrogolide hydrochloride
4.
Prodrugs
5.
1- Methyl- 4- phenyl- 1,2,3,6- tetrahydropyridine (MPTP)
6.
Levodopa (L Dopa)
7.
Diacetyl (Biacetyl)
8.
A 77636
9.
phenanthrene
Related Therapies and Procedures
1.
Therapeutics