SB-277011
Based on 1 publication(s) in Google Scholar
SB-277011 (SB-277011A) is a highly selective dopamine D3 receptor antagonist. SB-277011 induces ejaculation delay by inhibiting the expulsion phase of ejaculation, without impairing ejaculatory secretion or erectile function. SB-277011 also prolongs the post-ejaculatory refractory period. SB-277011 has no effect on the spontaneous preference of male rats for females in the sexually receptive phase. SB-277011 is widely applicable to studies related to premature ejaculation.
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- No. CAS: 215803-78-4
- Fòrmula: C28H30N4O
- Peso molecular:438.56
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Publications Citing Use of MedChemExpress (MCE) SB-277011
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Actividad biológica
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D3 Receptor |
SB-277011 (1-10 mg/kg; i.p.; single dose) does not impair sexual incentive motivation or locomotor activity in male rats at doses up to 10 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Han Wistar (male, 300-360 g, 7-OH-DPAT-induced ejaculation model)[2]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Reduced the mean number of ejaculations from 1.4 to 0.4 at 10 mg/kg.
Increased the latency to first ejaculation from 64 to 417 seconds at 10 mg/kg.
Increased the latency to first bulbospongiosus muscle response from 60 to 322 seconds at 10 mg/kg.
Caused a dose-dependent increase in the proportion of incomplete sexual responses, with a 6-fold increase at 10 mg/kg.
Did not alter the number, latency, amplitude, or duration of seminal vesicle pressure or intracavernous pressure responses at any dose.
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Animal Model:Han Wistar (male, 300-325 g; ovariectomized female, 225-250 g, sexual incentive motivation model)[2]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Had no significant effect on time spent in the sexual incentive zone, time spent in the social incentive zone, number of visits to either zone, or locomotor activity (distance moved, velocity) at any tested dose.
Maintained a significant preference for the sexual incentive over the social incentive in all treatment groups.
Chemical Information
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No. CAS 215803-78-4
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Peso molecular 438.56
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Fòrmula C28H30N4O
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SMILES
O=C(C1=CC=NC2=CC=CC=C21)N[C@@H]3CC[C@H](CC3)CCN4CC5=C(CC4)C=C(C#N)C=C5
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Synonyms
SB-277011A
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Neurosci
Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties. [Abstract]2022 Jan;25(1):39-49. PMID: 34887590
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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