Agonistic actions of pergolide on firing activity of dopamine neurons in substantia nigra compacta area. 1995

X X Zhang, and G Z Jin, and Y F Wei
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.

OBJECTIVE To study the potency of pergolide as a D2 receptor agonist on the firing activity of substantia nigra compacta (SNC) dopamine (DA) neurons compared with that of bromocriptine and to determine whether pergolide has the nature of D1 receptor agonist in vivo. METHODS Extracellular single unit recording techniques. RESULTS Both pergolide and bromocriptine decreased the spontaneously firing rate of "sensitive" and "insensitive" DA cells. In regard of ID50 values, pergolide (11.9, 95% fiducial limits, 5.7-25.1 micrograms kg-1) was more potent than bromocriptine (7.8, 95% fiducial limits, 3.3-18.5 mg kg-1). The discharge inhibition of pergolide was attenuated following the injection of selective D2 receptor antagonist spiperone 0.25 mg kg-1 or selective D1 receptor antagonist Sch-23390 1-2 mg kg-1. However, the inhibition caused by bromocriptine was not always attenuated by spiperone. CONCLUSIONS Pergolide is 650 times more potent than bromocriptine at D2 receptors, and possesses D1 receptor agonist characteristics in vivo.

UI MeSH Term Description Entries
D008297 Male Males
D009474 Neurons The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM. Nerve Cells,Cell, Nerve,Cells, Nerve,Nerve Cell,Neuron
D010479 Pergolide A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES. Celance,LY-127,809,LY-127809,Parkotil,Pergolide Mesylate,Permax,Pharken,LY127,809,LY127809,Mesylate, Pergolide
D001971 Bromocriptine A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion. 2-Bromoergocryptine,Bromocryptin,2-Bromo-alpha-ergocryptine,2-Bromo-alpha-ergokryptine,2-Bromoergocryptine Mesylate,2-Bromoergocryptine Methanesulfonate,2-Bromoergokryptine,Bromocriptin,Bromocriptine Mesylate,CB-154,Parlodel,2 Bromo alpha ergocryptine,2 Bromo alpha ergokryptine,2 Bromoergocryptine,2 Bromoergocryptine Mesylate,2 Bromoergocryptine Methanesulfonate,2 Bromoergokryptine,CB 154,CB154,Mesylate, 2-Bromoergocryptine,Mesylate, Bromocriptine,Methanesulfonate, 2-Bromoergocryptine
D004594 Electrophysiology The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013378 Substantia Nigra The black substance in the ventral midbrain or the nucleus of cells containing the black substance. These cells produce DOPAMINE, an important neurotransmitter in regulation of the sensorimotor system and mood. The dark colored MELANIN is a by-product of dopamine synthesis. Nigra, Substantia,Nigras, Substantia,Substantia Nigras
D017207 Rats, Sprague-Dawley A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company. Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats
D017447 Receptors, Dopamine D1 A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES. Dopamine D1 Receptors,Dopamine-D1 Receptor,D1 Receptors, Dopamine,Dopamine D1 Receptor,Receptor, Dopamine-D1
D017448 Receptors, Dopamine D2 A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES. Dopamine D2 Receptors,Dopamine-D2 Receptor,D2 Receptors, Dopamine,Dopamine D2 Receptor,Receptor, Dopamine-D2

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