Retinal dopaminergic receptor affinity and ocular pharmacokinetic profile of piribedil
Binding studies on retinal dopamine receptors have revealed the existence of both D1 and D2 receptors. Human retina micro-autoradiographs confirm the distribution of dopaminergic receptors in the plexiform layers. Piribedil, a dopaminergic agonist, is able to bind to D2 receptors, while its metaboli...
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| Veröffentlicht in: | Journal of neurology 1992-01, Vol.239 (S1), p.S17-S21 |
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| container_end_page | S21 |
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| container_issue | S1 |
| container_start_page | S17 |
| container_title | Journal of neurology |
| container_volume | 239 |
| creator | LAPALUS, P DENIS, P DRICI, M FREDJ-REYGROBELLET, D ELENA, P. P |
| description | Binding studies on retinal dopamine receptors have revealed the existence of both D1 and D2 receptors. Human retina micro-autoradiographs confirm the distribution of dopaminergic receptors in the plexiform layers. Piribedil, a dopaminergic agonist, is able to bind to D2 receptors, while its metabolite (S584) preferentially displaces D1-specific radioligands. These results demonstrate that piribedil has a dopamine-like pharmacological profile including direct interaction with receptors. When instilled into the rabbit eye, piribedil penetrates rapidly and accumulates in the pigmented epithelia--the iris ciliary body and chorioretina--before being rapidly cleared. Macro-autoradiographs confirm this distribution and show the levels to be compatible with the affinity of piribedil for retinal dopaminergic receptors. |
| doi_str_mv | 10.1007/BF00819562 |
| format | Article |
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Macro-autoradiographs confirm this distribution and show the levels to be compatible with the affinity of piribedil for retinal dopaminergic receptors.</description><identifier>ISSN: 0340-5354</identifier><identifier>EISSN: 1432-1459</identifier><identifier>DOI: 10.1007/BF00819562</identifier><identifier>PMID: 1634906</identifier><identifier>CODEN: JNRYA9</identifier><language>eng</language><publisher>Berlin: Springer</publisher><subject>Animals ; Anticonvulsants. Antiepileptics. Antiparkinson agents ; Autoradiography ; Biological and medical sciences ; Humans ; Medical sciences ; Neuropharmacology ; Pharmacology. 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Macro-autoradiographs confirm this distribution and show the levels to be compatible with the affinity of piribedil for retinal dopaminergic receptors.</description><subject>Animals</subject><subject>Anticonvulsants. Antiepileptics. Antiparkinson agents</subject><subject>Autoradiography</subject><subject>Biological and medical sciences</subject><subject>Humans</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Pharmacology. 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Antiparkinson agents</topic><topic>Autoradiography</topic><topic>Biological and medical sciences</topic><topic>Humans</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Piribedil - pharmacokinetics</topic><topic>Rabbits</topic><topic>Receptors, Dopamine - metabolism</topic><topic>Retina - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>LAPALUS, P</creatorcontrib><creatorcontrib>DENIS, P</creatorcontrib><creatorcontrib>DRICI, M</creatorcontrib><creatorcontrib>FREDJ-REYGROBELLET, D</creatorcontrib><creatorcontrib>ELENA, P. 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P</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Retinal dopaminergic receptor affinity and ocular pharmacokinetic profile of piribedil</atitle><jtitle>Journal of neurology</jtitle><addtitle>J Neurol</addtitle><date>1992-01</date><risdate>1992</risdate><volume>239</volume><issue>S1</issue><spage>S17</spage><epage>S21</epage><pages>S17-S21</pages><issn>0340-5354</issn><eissn>1432-1459</eissn><coden>JNRYA9</coden><abstract>Binding studies on retinal dopamine receptors have revealed the existence of both D1 and D2 receptors. Human retina micro-autoradiographs confirm the distribution of dopaminergic receptors in the plexiform layers. Piribedil, a dopaminergic agonist, is able to bind to D2 receptors, while its metabolite (S584) preferentially displaces D1-specific radioligands. These results demonstrate that piribedil has a dopamine-like pharmacological profile including direct interaction with receptors. 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| identifier | ISSN: 0340-5354 |
| ispartof | Journal of neurology, 1992-01, Vol.239 (S1), p.S17-S21 |
| issn | 0340-5354 1432-1459 |
| language | eng |
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| source | MEDLINE; Springer Nature - Complete Springer Journals |
| subjects | Animals Anticonvulsants. Antiepileptics. Antiparkinson agents Autoradiography Biological and medical sciences Humans Medical sciences Neuropharmacology Pharmacology. Drug treatments Piribedil - pharmacokinetics Rabbits Receptors, Dopamine - metabolism Retina - metabolism |
| title | Retinal dopaminergic receptor affinity and ocular pharmacokinetic profile of piribedil |
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