MovDisordV3, Main, Exploration, bibRecord, 005B26

N‐0923, a selective dopamine D2 receptor agonist, is efficacious in rat and monkey models of Parkinson's disease

Identifieur interne : 005B26 ( Main/Exploration ); précédent : 005B25; suivant : 005B27

N‐0923, a selective dopamine D2 receptor agonist, is efficacious in rat and monkey models of Parkinson's disease

Auteurs : Belluzzi [États-Unis] ; E. F. Domino [États-Unis] ; J. M. May [États-Unis] ; K. S. Bankiewicz [États-Unis] ; D. A. Mcafee [États-Unis]

Source :

Movement Disorders [ 0885-3185 ] ; 1994.

RBID : ISTEX:2B05DA604196BD25510BAB9ECB73B593B7B01D6F

English descriptors

KwdEn :
- (+)‐PHNO, 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (pharmacology), Animals, Bromocriptine (pharmacology), Disease Models, Animal, Dominance, Cerebral (drug effects), Dominance, Cerebral (physiology), Dopamine Agents (pharmacology), Dopamine D2 receptor agonists, Female, Hemiparkinsonian monkeys, Injections, Intramuscular, Macaca nemestrina, Male, N‐0923, Oxazines (pharmacology), Oxidopamine (pharmacology), Parkinson Disease, Secondary (chemically induced), Parkinson Disease, Secondary (physiopathology), Parkinson's disease, Prolactin (blood), Rat rotation, Rats, Rats, Sprague-Dawley, Receptors, Dopamine D2 (drug effects), Receptors, Dopamine D2 (physiology), Stereotyped Behavior (drug effects), Stereotyped Behavior (physiology), Substantia Nigra (drug effects), Substantia Nigra (physiopathology), Tetrahydronaphthalenes (pharmacology), Thiophenes (pharmacology).
MESH :
- chemical , blood : Prolactin.
- chemical , drug effects : Receptors, Dopamine D2.
- chemical , pharmacology : 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine, Bromocriptine, Dopamine Agents, Oxazines, Oxidopamine, Tetrahydronaphthalenes, Thiophenes.
- chemically induced : Parkinson Disease, Secondary.
- drug effects : Dominance, Cerebral, Stereotyped Behavior, Substantia Nigra.
- physiology : Dominance, Cerebral, Receptors, Dopamine D2, Stereotyped Behavior.
- physiopathology : Parkinson Disease, Secondary, Substantia Nigra.
- Animals, Disease Models, Animal, Female, Injections, Intramuscular, Macaca nemestrina, Male, Rats, Rats, Sprague-Dawley.

Abstract

Certain aminotetralins are known to be potent dopamine D2 receptor agonists. N‐0923, [‐]2‐(N‐propyl‐N‐2‐thienylethylamino)‐5‐hydroxytetralin HCl, recognizes the high and low affinity states of the D2 receptor in membranes from bovine caudate with a Klow of 79 nM. The selectivity ratio is D2/D1 = 15 and D2/α2 = 1.4. N‐0923 also inhibits dopamine uptake and prolactin secretion, and it is an antagonist at the α2 receptor. N‐0923 (3–300 nmol/kg, s.c.) induced dose‐dependent contralateral turning behavior in rats with unilateral 6‐hydroxydopamine lesions of the substantia nigra. The ED50 of 30 nmol/kg was effective for 1 h. The positive enantiomer (N‐0924; 300 nmol/kg, s. c.) was without effect. A hemiparkinsonian syndrome was induced in four Macaca nemestrina monkeys by unilateral infusion of the neurotoxin MPTP into the right carotid artery. Video recordings of free‐moving behavior revealed bradykinesia, disuse of the contralateral upper limb and turning in a direction ipsilateral to the lesion. N‐0923 (3–300 nmol/kg, i.m.) induced contralateral turning behavior, exploratory activity, and contralateral limb usage. The ED50 for turning (30 nmol/kg) was effective for 0.5 h. The potency order for induction of contralateral rotations was (+)‐PHNON‐0923 > bromocriptine. N‐0924 (300 nmol/kg, i. m.) was ineffective. We conclude that N‐0923 may be useful as a therapeutic agent in the treatment of Parkinson's disease.

Url:

https://api.istex.fr/document/2B05DA604196BD25510BAB9ECB73B593B7B01D6F/fulltext/pdf

DOI: 10.1002/mds.870090204

Affiliations:

Le document en format XML

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<author><name sortKey="Domino, E F" sort="Domino, E F" uniqKey="Domino E" first="E. F." last="Domino">E. F. Domino</name>
</author>
<author><name sortKey="May, J M" sort="May, J M" uniqKey="May J" first="J. M." last="May">J. M. May</name>
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<author><name sortKey="Bankiewicz, K S" sort="Bankiewicz, K S" uniqKey="Bankiewicz K" first="K. S." last="Bankiewicz">K. S. Bankiewicz</name>
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<author><name sortKey="May, J M" sort="May, J M" uniqKey="May J" first="J. M." last="May">J. M. May</name>
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<series><title level="j">Movement Disorders</title>
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<term>1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (pharmacology)</term>
<term>Animals</term>
<term>Bromocriptine (pharmacology)</term>
<term>Disease Models, Animal</term>
<term>Dominance, Cerebral (drug effects)</term>
<term>Dominance, Cerebral (physiology)</term>
<term>Dopamine Agents (pharmacology)</term>
<term>Dopamine D2 receptor agonists</term>
<term>Female</term>
<term>Hemiparkinsonian monkeys</term>
<term>Injections, Intramuscular</term>
<term>Macaca nemestrina</term>
<term>Male</term>
<term>N‐0923</term>
<term>Oxazines (pharmacology)</term>
<term>Oxidopamine (pharmacology)</term>
<term>Parkinson Disease, Secondary (chemically induced)</term>
<term>Parkinson Disease, Secondary (physiopathology)</term>
<term>Parkinson's disease</term>
<term>Prolactin (blood)</term>
<term>Rat rotation</term>
<term>Rats</term>
<term>Rats, Sprague-Dawley</term>
<term>Receptors, Dopamine D2 (drug effects)</term>
<term>Receptors, Dopamine D2 (physiology)</term>
<term>Stereotyped Behavior (drug effects)</term>
<term>Stereotyped Behavior (physiology)</term>
<term>Substantia Nigra (drug effects)</term>
<term>Substantia Nigra (physiopathology)</term>
<term>Tetrahydronaphthalenes (pharmacology)</term>
<term>Thiophenes (pharmacology)</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="blood" xml:lang="en"><term>Prolactin</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="drug effects" xml:lang="en"><term>Receptors, Dopamine D2</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine</term>
<term>Bromocriptine</term>
<term>Dopamine Agents</term>
<term>Oxazines</term>
<term>Oxidopamine</term>
<term>Tetrahydronaphthalenes</term>
<term>Thiophenes</term>
</keywords>
<keywords scheme="MESH" qualifier="chemically induced" xml:lang="en"><term>Parkinson Disease, Secondary</term>
</keywords>
<keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Dominance, Cerebral</term>
<term>Stereotyped Behavior</term>
<term>Substantia Nigra</term>
</keywords>
<keywords scheme="MESH" qualifier="physiology" xml:lang="en"><term>Dominance, Cerebral</term>
<term>Receptors, Dopamine D2</term>
<term>Stereotyped Behavior</term>
</keywords>
<keywords scheme="MESH" qualifier="physiopathology" xml:lang="en"><term>Parkinson Disease, Secondary</term>
<term>Substantia Nigra</term>
</keywords>
<keywords scheme="MESH" xml:lang="en"><term>Animals</term>
<term>Disease Models, Animal</term>
<term>Female</term>
<term>Injections, Intramuscular</term>
<term>Macaca nemestrina</term>
<term>Male</term>
<term>Rats</term>
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<front><div type="abstract" xml:lang="en">Certain aminotetralins are known to be potent dopamine D2 receptor agonists. N‐0923, [‐]2‐(N‐propyl‐N‐2‐thienylethylamino)‐5‐hydroxytetralin HCl, recognizes the high and low affinity states of the D2 receptor in membranes from bovine caudate with a Klow of 79 nM. The selectivity ratio is D2/D1 = 15 and D2/α2 = 1.4. N‐0923 also inhibits dopamine uptake and prolactin secretion, and it is an antagonist at the α2 receptor. N‐0923 (3–300 nmol/kg, s.c.) induced dose‐dependent contralateral turning behavior in rats with unilateral 6‐hydroxydopamine lesions of the substantia nigra. The ED50 of 30 nmol/kg was effective for 1 h. The positive enantiomer (N‐0924; 300 nmol/kg, s. c.) was without effect. A hemiparkinsonian syndrome was induced in four Macaca nemestrina monkeys by unilateral infusion of the neurotoxin MPTP into the right carotid artery. Video recordings of free‐moving behavior revealed bradykinesia, disuse of the contralateral upper limb and turning in a direction ipsilateral to the lesion. N‐0923 (3–300 nmol/kg, i.m.) induced contralateral turning behavior, exploratory activity, and contralateral limb usage. The ED50 for turning (30 nmol/kg) was effective for 0.5 h. The potency order for induction of contralateral rotations was (+)‐PHNON‐0923 > bromocriptine. N‐0924 (300 nmol/kg, i. m.) was ineffective. We conclude that N‐0923 may be useful as a therapeutic agent in the treatment of Parkinson's disease.</div>
</front>
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<li>Michigan</li>
<li>Virginie</li>
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<tree><country name="États-Unis"><region name="Virginie"><name sortKey="Belluzzi" sort="Belluzzi" uniqKey="Belluzzi" last="Belluzzi">Belluzzi</name>
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Movement Disorders (revue)

N‐0923, a selective dopamine D2 receptor agonist, is efficacious in rat and monkey models of Parkinson's disease

N‐0923, a selective dopamine D2 receptor agonist, is efficacious in rat and monkey models of Parkinson's disease

Source :

English descriptors

Abstract

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	Movement Disorders (revue)
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