SB-277011

SB-277011 (SB-277011A) is a Dopamine D3 receptor antagonist

The selective dopamine D3 receptor antagonist SB 277011-A, but not the partial agonist BP 897, blocks cue-induced reinstatement of nicotine-seeking.[Pubmed:19995481]

Int J Neuropsychopharmacol. 2010 Mar;13(2):181-90.

The dopamine D3 receptor (DRD3) has been suggested to be involved in the mechanisms underlying stimulus-controlled drug-seeking behaviour. Ligands acting as DRD3 antagonists (SB 277011-A) or DRD3 partial agonists (BP 897) have shown some promise for reducing the influence of drug-associated cues on motivational behaviour. Here, effects of SB 277011-A and BP 897 were evaluated on cue-induced reinstatement of nicotine-seeking in rats. The effects of BP 897 on nicotine self-administration under a fixed-ratio 5 (FR5) schedule of reinforcement were also evaluated. SB 277011-A (1-10 mg/kg) was able to block cue-induced reinstatement of nicotine-seeking, indicating that DRD3 selective antagonism may be an effective approach to prevent relapse for nicotine. In contrast, BP 897 did not block the cue-induced reinstatement of nicotine-seeking or nicotine-taking under the FR5 schedule. In a control study, rats did not respond to the light stimuli without nicotine delivery, indicating that the responding for the drug-associated cues was induced by the previous pairing of light stimuli with nicotine's effects. These findings validate the role of DRD3 on reactivity to drug-associated stimuli and suggest that the DRD3 antagonist, but perhaps not the DRD3 partial agonist, could be used to prevent relapse in tobacco smokers.

Delay of ejaculation induced by SB-277011, a selective dopamine D3 receptor antagonist, in the rat.[Pubmed:19207271]

J Sex Med. 2009 Apr;6(4):980-988.

INTRODUCTION: Dopamine (DA) plays a key role in different aspects of the male sexual response, including sexual motivation and arousal, penile erection, and ejaculation. The modalities of action of DA are however unclear, although the various DA receptors may differentially mediate the activity of DA in different aspects of the male sexual response. AIM: To clarify the role of DA D(3) receptors in the control of the male sexual response. METHODS: The effects of a highly selective DA D(3) receptors antagonist (SB-277011; intraperitoneal) were tested in experimental paradigms exploring several aspects of the male sexual response in (i) anesthetized rats using 7-hydroxy-N,N-di-n-propylaminotetralin to induce ejaculation and (ii) conscious rats using sexual incentive motivation and mating tests. MAIN OUTCOME MEASURES: Physiological markers of erection and emission and expulsion phases of ejaculation were measured in anesthetized rats. Behavioral parameters of sexual incentive motivation and mating tests were quantified. RESULTS: In anesthetized rats, we found that SB-277011 specifically and dose-dependently inhibited the expulsion phase of ejaculation without impairing either emission phase or erection, and this resulted in delayed ejaculation. Administration of SB-277011 had no effect on the spontaneous preference that males displayed for sexually receptive females as shown in sexual incentive motivation test. Delayed ejaculation was confirmed when male rats were administered with the highest dose of SB-277011 (10 mg/kg) in mating test, where males were free to copulate with estrous females. In addition, the refractory period following ejaculation was lengthened in rats treated with SB-277011. CONCLUSION: As a whole, the present data demonstrate the specific and primary role of D(3) receptors in the expulsion phase of ejaculation and provide preclinical evidence for the investigation of the therapeutic potential of D(3) antagonism for treating premature ejaculation.

Selective D3 Receptor Antagonist SB-277011-A Potentiates the Effect of Cocaine on Extracellular Dopamine in the Nucleus Accumbens: a Dual Core-Shell Voltammetry Study in Anesthetized Rats.[Pubmed:27873908]

Sensors (Basel). 2008 Nov 4;8(11):6936-6951.

Dopamine (DA) D3 receptors have been associated with drug intake and abuse and selectively distribute in the brain circuits responding to drug administration. Here we examined the effects of an acute systemic administration of cocaine (15 mg/kg) alone or preceded by treatment with the selective D3 receptor antagonist SB-277011-A (10 mg/kg) on DA levels concurrently in the rat nucleus accumbens shell and core sub-regions (NAcshell and NAccore, respectively). It is shown that cocaine increases extracellular DA in both compartments and that blocking D3 receptors with SB-277011-A, although the latter is devoid of dopaminergic effects per se, potentiates these effects. No differences in the amplitude of the response were observed between NAcshell and NAccore compartments, though the dopaminergic response in the NAcshell was transient whereas that in the NAccore rose slowly to reach a plateau. These results demonstrate the feasibility to use multiprobe voltammetry to measure discrete monoaminergic responses in discrete areas of the brain and confirm the effect of D3 receptors antagonist at modifying the neurochemical effects of cocaine.

The selective dopamine D(3) receptor antagonist SB-277011-A significantly decreases binge-like consumption of ethanol in C57BL/J6 mice.[Pubmed:25764479]

Synapse. 2015 Jun;69(6):295-8.

The authors show that the dopamine D3 antagonist SB-277011-A consistently and persistently decrease binge-like EtOH consumption at 30 mg/kg and it decreases binge-like consumption on days 3, 7, 9, and 11-13 at 15 mg/kg. These findings suggest that the brain's D3 receptor may also be involved in not only ethanol reward but binge drinking as well.

SB-277011 is a potent and delective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively); brain penetrant.

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