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Identifiers | |
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CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.162.446 |
Chemical and physical data | |
Formula | C4H8N2O2 |
Molar mass | 116.120 g·mol−1 |
3D model ( JSmol) | |
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HA-966 or (±)-3-amino-1-hydroxy-pyrrolidin-2-one is a molecule used in scientific research as a glycine receptor and NMDA receptor antagonist / low efficacy partial agonist. It has neuroprotective and anticonvulsant, [1] anxiolytic, [2] antinociceptive [3] and sedative / hypnotic [4] effects in animal models. Pilot human clinical trials in the early 1960s showed that HA-966 appeared to benefit patients with tremors of extrapyramidal origin. [4]
The two enantiomers of HA-966 have differing pharmacological activity. The glycine/N-methyl-D-aspartate receptor antagonist activity is specific to the (R)-(+)-enantiomer, whereas the sedative and ataxic effects are specific to the (S)-(-)-enantiomer. [5]
(R)-(+)-HA-966 did not induce drug-appropriate responding in animals trained to discriminate phencyclidine (PCP) from saline, suggesting that the glycine receptor ligand (R)-(+)-HA-966 has a significantly different behavioral profile than drugs affecting the ion channel of the NMDA receptor complex. [6]
(S)-(-)-HA-966 has been described as a " γ-hydroxybutyric acid (GHB)-like agent" [7] and a "potent y-butyrolactone-like sedative", [5] but it shows no affinity for the GABAB receptor (GABABR). [7]
![]() | |
Identifiers | |
---|---|
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.162.446 |
Chemical and physical data | |
Formula | C4H8N2O2 |
Molar mass | 116.120 g·mol−1 |
3D model ( JSmol) | |
| |
|
HA-966 or (±)-3-amino-1-hydroxy-pyrrolidin-2-one is a molecule used in scientific research as a glycine receptor and NMDA receptor antagonist / low efficacy partial agonist. It has neuroprotective and anticonvulsant, [1] anxiolytic, [2] antinociceptive [3] and sedative / hypnotic [4] effects in animal models. Pilot human clinical trials in the early 1960s showed that HA-966 appeared to benefit patients with tremors of extrapyramidal origin. [4]
The two enantiomers of HA-966 have differing pharmacological activity. The glycine/N-methyl-D-aspartate receptor antagonist activity is specific to the (R)-(+)-enantiomer, whereas the sedative and ataxic effects are specific to the (S)-(-)-enantiomer. [5]
(R)-(+)-HA-966 did not induce drug-appropriate responding in animals trained to discriminate phencyclidine (PCP) from saline, suggesting that the glycine receptor ligand (R)-(+)-HA-966 has a significantly different behavioral profile than drugs affecting the ion channel of the NMDA receptor complex. [6]
(S)-(-)-HA-966 has been described as a " γ-hydroxybutyric acid (GHB)-like agent" [7] and a "potent y-butyrolactone-like sedative", [5] but it shows no affinity for the GABAB receptor (GABABR). [7]