2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. SB-277011

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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SB-277011

SB-277011 Chemical Structure

CAS No. : 215803-78-4

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Description

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[1][2].

IC50 & Target[1]

D3 Receptor

 

In Vivo

SB-277011 (1-10 mg/kg; i.p.) dose-dependently inhibits the expulsion phase of ejaculation in 7-OH-DPAT-challenged anesthetized male Wistar rats, delaying ejaculation without affecting erection or emission[1].
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.

Animal Model: Han Wistar (male, 300-360 g, 7-OH-DPAT-induced ejaculation model)[2]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose
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.
Animal Model: Han Wistar (male, 300-325 g; ovariectomized female, 225-250 g, sexual incentive motivation model)[2]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose
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.
Molecular Weight

438.56

Formula

C28H30N4O
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Keywords:

SB-277011215803-78-4SB-277011ASB277011SB 277011Dopamine Receptoremissionmale sexual responsesexual incentive motivationmale Wistar ratspost-ejaculatory refractory perioderectionpremature ejaculationlocomotor activityejaculationdopamine D3 receptorInhibitorinhibitorinhibit

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