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编 号：F295090
分子式：C32H40BrN5O5
分子量：654.59
分子式：C32H40BrN5O5
分子量：654.59
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CAS No: 25614-03-3
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生物活性：
Bromocriptine is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.
体内研究：
Bromocriptine (a dopamine agonist) treatment (2 mg/kg, i.p.) group shows significant anti-immobility action as compared to control. When Bromocriptine administered 30 min after the last dose of 7 days MPE treatment and subjected to FST, this dopaminergic agonist produces significant and dose dependent potentiation of anti-immobility action of MPE (200 mg/kg, p.o.) as compared to MPE treatment alone. Bromocriptine (a dopamine agonist) treatment (2 mg/kg, i.p.) group shows a significant reduction of immobility time as compared to control. Bromocriptine administration after 7 days pretreatment with MPE (100 and 200 mg/kg, p.o.) shows significant and dose dependent potentiation of anti-immobility action of MPE as compared to MPE treatment alone. Intraperitoneal administration of Bromocriptine induces a significant, dose dependent (0.1 mg and 1 mg/Kg) decrease in pain scores in CCI-IoN group when compared to sham and its effect lasted for 6 h. The highest dose induces the highest score decrease, (P<0.01). As a positive control SKF8129 (DR1 agonist) is used. Its intraperitoneal administration induces a non-significant increase in the SMA score when compared to sham (saline-injected). Intracisternal administration of Bromocriptine decreases significantly the SMA score when compared to sham (saline-injected). Bromocriptine effect lasted for 20 min. Intraperitoneal administration of Bromocriptine induces a significant dose dependent decrease in SMA score in CCI-IoN?+?6-OHDA lesioned group compared to that of sham. Its effect lasted for 6 h. SKF81297 administration increases the allodynic score. Intracisternal administration of Bromocriptine decreases significantly the SMA score compared to that of sham (saline-injected rats) and its effect lasted for 30 min.
体外研究：
Bromocriptine stimulates [35S]-GTPγS binding at D2 dopamine receptor expressed in CHO cells with pEC50 of 8.15±0.05. Bromocriptine also is a strong inhibitor of brain nitric oxide synthase. The ergot alkaloid Bromocriptine (BKT) is found to act as a strong inhibitor of purified neuronal nitric oxide synthase (NOS) (IC50=10±2 μM) whereas it is poorly active towards inducible macrophage NOS (IC50>100 μM) . Bromocriptine is found to inhibit the activity of at least one human cytochrome P450 enzyme. Bromocriptine is a potent inhibitor of CYP3A4 with a calculated IC50 value for the interaction of 1.69 μM.
Bromocriptine is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.
体内研究：
Bromocriptine (a dopamine agonist) treatment (2 mg/kg, i.p.) group shows significant anti-immobility action as compared to control. When Bromocriptine administered 30 min after the last dose of 7 days MPE treatment and subjected to FST, this dopaminergic agonist produces significant and dose dependent potentiation of anti-immobility action of MPE (200 mg/kg, p.o.) as compared to MPE treatment alone. Bromocriptine (a dopamine agonist) treatment (2 mg/kg, i.p.) group shows a significant reduction of immobility time as compared to control. Bromocriptine administration after 7 days pretreatment with MPE (100 and 200 mg/kg, p.o.) shows significant and dose dependent potentiation of anti-immobility action of MPE as compared to MPE treatment alone. Intraperitoneal administration of Bromocriptine induces a significant, dose dependent (0.1 mg and 1 mg/Kg) decrease in pain scores in CCI-IoN group when compared to sham and its effect lasted for 6 h. The highest dose induces the highest score decrease, (P<0.01). As a positive control SKF8129 (DR1 agonist) is used. Its intraperitoneal administration induces a non-significant increase in the SMA score when compared to sham (saline-injected). Intracisternal administration of Bromocriptine decreases significantly the SMA score when compared to sham (saline-injected). Bromocriptine effect lasted for 20 min. Intraperitoneal administration of Bromocriptine induces a significant dose dependent decrease in SMA score in CCI-IoN?+?6-OHDA lesioned group compared to that of sham. Its effect lasted for 6 h. SKF81297 administration increases the allodynic score. Intracisternal administration of Bromocriptine decreases significantly the SMA score compared to that of sham (saline-injected rats) and its effect lasted for 30 min.
体外研究：
Bromocriptine stimulates [35S]-GTPγS binding at D2 dopamine receptor expressed in CHO cells with pEC50 of 8.15±0.05. Bromocriptine also is a strong inhibitor of brain nitric oxide synthase. The ergot alkaloid Bromocriptine (BKT) is found to act as a strong inhibitor of purified neuronal nitric oxide synthase (NOS) (IC50=10±2 μM) whereas it is poorly active towards inducible macrophage NOS (IC50>100 μM) . Bromocriptine is found to inhibit the activity of at least one human cytochrome P450 enzyme. Bromocriptine is a potent inhibitor of CYP3A4 with a calculated IC50 value for the interaction of 1.69 μM.
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