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(R)-(+)-HA-966

(R)-(+)-HA-966

Catalog No. BCC6588
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10mg $141.00 Ship Within 7 Days
50mg $599.00 Ship Within 7 Days
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Quality Control of (R)-(+)-HA-966

Chemical structure

(R)-(+)-HA-966

Biological Activity of (R)-(+)-HA-966

Antagonist/partial agonist at the glycine site of the NMDA receptor; able to cross the blood-brain barrier. Also available as part of the NMDA Receptor - Glycine Site. S-enantiomer available.

(R)-(+)-HA-966 Dilution Calculator

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Chemical Properties of (R)-(+)-HA-966

Cas No. 123931-04-4 SDF Download SDF
Chemical Name (R)-(+)-3-Amino-1-hydroxypyrrolidin-2-one
SMILES C1CN(C(=O)C1N)O
Standard InChIKey HCKUBNLZMKAEIN-GSVOUGTGSA-N
Standard InChI InChI=1S/C4H8N2O2/c5-3-1-2-6(8)4(3)7/h3,8H,1-2,5H2/t3-/m1/s1
Formula C4H8N2O2 M.Wt 116.12
Solubility Soluble to 100 mM in water
Storage Desiccate at RT
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other courier with RT , or blue ice upon request.

Preparing Stock Solutions of (R)-(+)-HA-966

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 8.6118 mL 43.0589 mL 86.1178 mL 172.2356 mL 215.2945 mL
5 mM 1.7224 mL 8.6118 mL 17.2236 mL 34.4471 mL 43.0589 mL
10 mM 0.8612 mL 4.3059 mL 8.6118 mL 17.2236 mL 21.5295 mL
50 mM 0.1722 mL 0.8612 mL 1.7224 mL 3.4447 mL 4.3059 mL
100 mM 0.0861 mL 0.4306 mL 0.8612 mL 1.7224 mL 2.1529 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

References on (R)-(+)-HA-966

Biochemical and behavioral anxiolytic-like effects of R(+)HA-966 at the level of the ventral tegmental area in rats.[Pubmed: 10353424]


R(+) HA-966, a weak partial agonist at the glycine/NMDA receptor complex, has been shown to have anxiolytic-like actions on restraint stress-induced mesoprefrontal dopamine metabolism.

Neuroprotective effects of the strychnine-insensitive glycine site NMDA antagonist (R)-HA-966 in an experimental model of Parkinson's disease.[Pubmed: 9219856]


The neuroprotective effects of (R)-HA-966 and (S)-HA-966 (3-amino-1-hydroxy-2-pyrrolidinone) were examined in an MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine)-induced animal model of Parkinson's disease. Systemic pretreatment of C57 black mice with the strychnine-insensitive glycine site antagonist, (R)-HA-966 (3-30 mg/kg, i.p.), dose-dependently attenuated MPTP-induced depletion of striatal dopamine and 3,4-dihydroxyphenylacetic acid (DOPAC). Pretreatment with (R)-HA-966 also significantly protected the degeneration of tyrosine hydroxylase-positive neurons in the substantia nigra of mice treated with MPTP and alleviated the acute behavioral changes caused by the neurotoxin. In contrast, the other racemic form, (S)-HA-966, neither prevented the neurochemical depletions nor the neuronal injury caused by MPTP. These results indicate that excitatory mechanisms of neurodegeneration are involved in the pathophysiology of Parkinson's disease, and that strychnine-insensitive glycine site NMDA antagonists may serve as dopaminoprotective agents which intervene in the progressive neurodegeneration in Parkinson's disease.

Discriminative stimulus effects of R-(+)-3-amino-1-hydroxypyrrolid-2-one, [(+)-HA-966], a partial agonist of the strychnine-insensitive modulatory site of the N-methyl-D-aspartate receptor.[Pubmed: 8531091]


The strychnine-insensitive glycine site on the N-methyl-D-aspartate (NMDA) receptor complex is a target for development of a host of therapeutic agents including anxiolytics, antidepressants, antiepileptics, anti-ischemics and cognitive enhancers. In the present experiments, the discriminative stimulus effects of (+)-HA-966 [R-(+)-3-amino-1-hydroxypyrrolid-2-one], a low-efficacy partial agonist of the glycine site, was explored. Male, Swiss-Webster mice were trained to discriminate (+)-HA-966 (170 mg/kg i.p.) from saline in a T-maze under which behavior was controlled by food. Other glycine partial agonists, 1-amino-1-cyclopropanecarboxilic acid and D-cycloserine, fully substituted for the discriminative stimulus effects of (+)-HA-966 despite known differences in other pharmacological effects of these compounds. The glycine site antagonist, 7-chlorkynurenic acid, did not substitute for (+)-HA-966. Likewise other functional NMDA antagonists acting at nonglycine sites of the NMDA receptor also did not substitute: neither the high (dizocilpine) or low affinity (ibogaine) ion-channel blocker, the competitive antagonist, NPC 17742 [2R,4R,5S-2-amino-4,5-(1, 2-cyclohexyl)-7-phosphonoheptanoic acid], nor the polyamine antagonist, ifenprodil, substituted for (+)-HA-966. Although the full agonist, glycine, did not substitute, this compound fully blocked the discriminative stimulus effects of (+)-HA-966. In a separate group of mice trained to discriminate 0.17 mg/kg of dizocilpine from saline, (+)-HA-966 produced a maximum of only 50% dizoclipine-appropriate responses. These data suggest that the discriminative stimulus effects of (+)-HA-966 are based upon its partial agonist actions at the strychnine-insensitive glycine site.(ABSTRACT TRUNCATED AT 250 WORDS)

R-(+)-HA-966, an antagonist for the glycine/NMDA receptor, prevents locomotor sensitization to repeated cocaine exposures.[Pubmed: 7757472]


Repeated administration of cocaine results in a reverse tolerance or sensitization to the locomotor stimulant properties of cocaine. In this study, we examined the effect of an antagonist for the strychinine-insensitive glycine receptor of the NMDA receptor complex, R-(+)-HA-966, on the development of locomotor sensitization to cocaine. Co-administration of R-(+)-HA-966 with repeated cocaine prevented locomotor sensitization to a subsequent challenge dose of cocaine. However, R-(+)-HA-966 (15 mg/kg i.p.) did not attenuate locomotor activation to an acute dose of cocaine (15 mg/kg). These results indicate that the glycine/NMDA receptor is involved in locomotor sensitization to repeated cocaine administration but not in the locomotor activation to the acute stimulant effects of cocaine administration.

Kewords:

(R)-(+)-HA-966,123931-04-4,Membrane Transporter/Ion Channel,NMDA Receptor, supplier, inhibitor,Antagonist,Blocker,Modulator,Agonist, activators, activates, potent, BioCrick

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