Dopamine agonists used in the treatment of Parkinson's disease and their selectivity for the D1, D2, and D3 dopamine receptors in human striatum

Sumanirole, a Highly Dopamine D2-Selective Receptor Agonist: In Vitro and in Vivo Pharmacological Characterization and Efficacy in Animal Models of Parkinson’s Disease

“…The affinity of sumanirole for D 2 receptors is 9.0 Ϯ 1.0 nM. This is similar to the affinity of D 2 receptors for ropinirole and slightly higher and lower than the receptor affinities for bromocriptine and pergolide, respectively, all agents used clinically for the treatment of Parkinson's disease (Eden et al, 1991;De Keyser et al, 1995;Rascol et al, 1996). The affinity of D 3 , D 4 , and D 1 receptors for sumanirole was calculated to be at least 200-fold lower than at D 2 receptors.…”

Sumanirole, a Highly Dopamine D2-Selective Receptor Agonist: In Vitro and in Vivo Pharmacological Characterization and Efficacy in Animal Models of Parkinson’s Disease

“…The affinity of sumanirole for D 2 receptors is 9.0 Ϯ 1.0 nM. This is similar to the affinity of D 2 receptors for ropinirole and slightly higher and lower than the receptor affinities for bromocriptine and pergolide, respectively, all agents used clinically for the treatment of Parkinson's disease (Eden et al, 1991;De Keyser et al, 1995;Rascol et al, 1996). The affinity of D 3 , D 4 , and D 1 receptors for sumanirole was calculated to be at least 200-fold lower than at D 2 receptors.…”

Identification of Novel Dopamine D2 Receptor Ligands—A Combined In Silico/In Vitro Approach

“…To generate a high-quality dataset for the generation of the pharmacophore models, highly active D 2 R ligands included in the ChEMBL database were compiled ( Figure 3 and Table S1 ) [ 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 , 68 , 69 , 70 ]. The final set included 68 active compounds.…”

Spatiotemporal Pattern of Striatal ERK1/2 Phosphorylation in a Rat Model of L-DOPA–Induced Dyskinesia and the Role of Dopamine D1 Receptors

“…We further showed that SCH 23390 was able to inhibit ERK1/2 and MSK-1 activation after a chronic course of L-DOPA treatment, which leads to internalization and possible desensitization of D1 receptors (Fiorentini et al 2006). Bromocriptine, an antiparkinsonian drug with strong motor-stimulating properties but no dyskinesiogenic potential (Lundblad et al 2002), exerting agonistic activity at D2 but not D1 receptors (Bedard et al 1993;De Keyser et al 1995), did not produce a significant activation of ERK1/2 and MSK-1 in the DA-denervated striatum. Taken together, these data indicate that D2 receptors are not implicated in the induction of ERK1/2-dependent signaling by L-DOPA, and support an association between ERK1/2 activation and the supersensitivity of D1 receptor-mediated signaling that follows DA denervation (Gerfen et al 2002).…”

Sumanirole, a Highly Dopamine D2-Selective Receptor Agonist: In Vitro and in Vivo Pharmacological Characterization and Efficacy in Animal Models of Parkinson’s Disease

“…The affinity of sumanirole for D 2 receptors is 9.0 Ϯ 1.0 nM. This is similar to the affinity of D 2 receptors for ropinirole and slightly higher and lower than the receptor affinities for bromocriptine and pergolide, respectively, all agents used clinically for the treatment of Parkinson's disease (Eden et al, 1991;De Keyser et al, 1995;Rascol et al, 1996). The affinity of D 3 , D 4 , and D 1 receptors for sumanirole was calculated to be at least 200-fold lower than at D 2 receptors.…”

Identification of Novel Dopamine D2 Receptor Ligands—A Combined In Silico/In Vitro Approach

“…To generate a high-quality dataset for the generation of the pharmacophore models, highly active D 2 R ligands included in the ChEMBL database were compiled ( Figure 3 and Table S1 ) [ 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 , 68 , 69 , 70 ]. The final set included 68 active compounds.…”

Spatiotemporal Pattern of Striatal ERK1/2 Phosphorylation in a Rat Model of L-DOPA–Induced Dyskinesia and the Role of Dopamine D1 Receptors

“…We further showed that SCH 23390 was able to inhibit ERK1/2 and MSK-1 activation after a chronic course of L-DOPA treatment, which leads to internalization and possible desensitization of D1 receptors (Fiorentini et al 2006). Bromocriptine, an antiparkinsonian drug with strong motor-stimulating properties but no dyskinesiogenic potential (Lundblad et al 2002), exerting agonistic activity at D2 but not D1 receptors (Bedard et al 1993;De Keyser et al 1995), did not produce a significant activation of ERK1/2 and MSK-1 in the DA-denervated striatum. Taken together, these data indicate that D2 receptors are not implicated in the induction of ERK1/2-dependent signaling by L-DOPA, and support an association between ERK1/2 activation and the supersensitivity of D1 receptor-mediated signaling that follows DA denervation (Gerfen et al 2002).…”

Sumanirole, a Highly Dopamine D2-Selective Receptor Agonist: In Vitro and in Vivo Pharmacological Characterization and Efficacy in Animal Models of Parkinson’s Disease

“…The affinity of sumanirole for D 2 receptors is 9.0 Ϯ 1.0 nM. This is similar to the affinity of D 2 receptors for ropinirole and slightly higher and lower than the receptor affinities for bromocriptine and pergolide, respectively, all agents used clinically for the treatment of Parkinson's disease (Eden et al, 1991;De Keyser et al, 1995;Rascol et al, 1996). The affinity of D 3 , D 4 , and D 1 receptors for sumanirole was calculated to be at least 200-fold lower than at D 2 receptors.…”

Identification of Novel Dopamine D2 Receptor Ligands—A Combined In Silico/In Vitro Approach

“…To generate a high-quality dataset for the generation of the pharmacophore models, highly active D 2 R ligands included in the ChEMBL database were compiled ( Figure 3 and Table S1 ) [ 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 , 68 , 69 , 70 ]. The final set included 68 active compounds.…”

Spatiotemporal Pattern of Striatal ERK1/2 Phosphorylation in a Rat Model of L-DOPA–Induced Dyskinesia and the Role of Dopamine D1 Receptors

“…We further showed that SCH 23390 was able to inhibit ERK1/2 and MSK-1 activation after a chronic course of L-DOPA treatment, which leads to internalization and possible desensitization of D1 receptors (Fiorentini et al 2006). Bromocriptine, an antiparkinsonian drug with strong motor-stimulating properties but no dyskinesiogenic potential (Lundblad et al 2002), exerting agonistic activity at D2 but not D1 receptors (Bedard et al 1993;De Keyser et al 1995), did not produce a significant activation of ERK1/2 and MSK-1 in the DA-denervated striatum. Taken together, these data indicate that D2 receptors are not implicated in the induction of ERK1/2-dependent signaling by L-DOPA, and support an association between ERK1/2 activation and the supersensitivity of D1 receptor-mediated signaling that follows DA denervation (Gerfen et al 2002).…”