| Bioactivity | (R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine[1][2]. (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain[3]. | |||||||||
| Target | glycine site of the NMDA receptor | |||||||||
| In Vivo | (R)-(+)-HA-966 ((+)-HA-966; 10 mg/kg; IV) significantly attenuates the dose-dependent pressor response and the associated tachycardic response elicited by systemic NMDA (125, 250, 500, and 1000 mg/kg; i.v.)[3]. (+)-HA-966 (30, 100 mg/kg; IP) dose-dependently blocks the enhancement of dopamine synthesis induced in the nucleus accumbens by amphetamine, but is without effect on the increase in dopamine synthesis in the striatum in male BKTO mice (20-30g)[1]. Animal Model: | |||||||||
| Name | (R)-(+)-HA-966 | |||||||||
| CAS | 123931-04-4 | |||||||||
| Formula | C4H8N2O2 | |||||||||
| Molar Mass | 116.12 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Hutson PH, et al. R-(+)-HA-966, a glycine/NMDA receptor antagonist, selectively blocks the activation of the mesolimbic dopamine system by amphetamine. Br J Pharmacol. 1991 Aug;103(4):2037-44. [2]. Witkin JM, et al. 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. J Pharmacol Exp Ther. 1995 Dec;275(3):1267-73. [3]. Christensen D, et al. The antinociceptive effect of combined systemic administration of morphine and the glycine/NMDA receptor antagonist, (+)-HA966 in a rat model of peripheral neuropathy. Br J Pharmacol. 1998 Dec;125(8):1641-50. |
(R)-(+)-HA-966
CAS: 123931-04-4 F: C4H8N2O2 W: 116.12
(R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor
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