Quinelorane hydrochloride - CAS 97548-97-5
Category: Inhibitor
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Molecular Weight:
Dopamine Receptor
Quinelorane hydrochloride, 2-aminopyridine analog of quinpirole, is a dopamine D2 and D3 receptor agonist (Ki= 5.7 and 3.4 nM respectively).
≥99% by HPLC
(5aR,9aR)-5,5a,6,7,8,9,9a,10-Octahydro-6-propyl-pyrido[2,3-g]quinazolin-2-amine Dihydrochloride; (5aR-trans)-5,5a,6,7,8,9,9a,10-Octahydro-6-propyl-pyrido[2,3-g]quinazolin-2-amine Dihydrochloride; LY 163502; LY163502; LY-163502
Store in a cool and dry place (or refer to the Certificate of Analysis).
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1.Age-related changes in the regulation of behavior by D-1:D-2 dopamine receptor interactions.
Murray AM;Waddington JL Neurobiol Aging. 1991 Sep-Oct;12(5):431-5.
Functional interactions between D-1 and D-2 dopamine receptor systems appear important in the regulation of psychomotor behavior, and may alter with aging. Male Sprague-Dawley rats of 5 and 20-24 months were challenged with the selective D-2 agonist LY 163502 alone or following pretreatment with the selective D-1 antagonist SCH 23390. Typical sniffing and locomotor responses to LY 163502 alone were significantly reduced in aged animals. Pretreatment with SCH 23390 blocked these typical responses in both young and aged animals, consistent with their regulation by cooperative D-1:D-2 interactions; however, SCH 23390 released a significant excess of atypical limb/body jerking to LY 163502 in aged animals, a response which appears to have its basis in oppositional D-1:D-2 interactions. These results suggest that the net effect of aging on dopaminergic transmission is to reduce tonic activity through D-1 receptors to a greater extent than that occurring through D-2 receptors. As the present aged animals showed a selective loss of striatal D-2 but not of D-1 receptors in radioligand binding studies, such a reduction of D-1-mediated transmission with aging would seem to involve loss of presynaptic function or of postsynaptic mechanisms beyond the D-1 recognition site.
2.Evidence that striatal synthesis-inhibiting autoreceptors are dopamine D3 receptors.
Meller E;Bohmaker K;Goldstein M;Basham DA Eur J Pharmacol. 1993 Nov 2;249(1):R5-6.
The activation constants (KA; dose required to occupy 50% of receptors) for reversal of gamma-butyrolactone (GBL)-induced elevation of striatal L-3,4-dihydroxyphenylalanine (L-DOPA) levels via stimulation of presynaptic dopamine receptors were determined for apomorphine and two dopamine D3 receptor-selective agonists, quinpirole and LY163502 (quinelorane). The KA values correlated significantly with the affinities (Ki) of the agonists for the D3 (r = 0.999, P < 0.05) but not the D2 (r = -0.13) receptor, suggesting that striatal synthesis-inhibiting autoreceptors are of the D3 rather than the D2 subtype.
3.Preclinical studies on quinelorane, a potent and highly selective D2-dopaminergic agonist.
Foreman MM;Fuller RW;Hynes MD;Gidda JS;Nichols CL;Schaus JM;Kornfeld EC;Clemens JA J Pharmacol Exp Ther. 1989 Jul;250(1):227-35.
Quinelorane (LY163502) has the endocrine, neurochemical and behavioral profile of a potent and highly selective D2-dopaminergic agonist. The administration of quinelorane produced dose-related decreases in serum prolactin concentration of reserpinized, male rats and increases in serum corticosterone concentration of male rats. The minimum effective doses (MED) for these effects were 10 and 30 micrograms/kg i.p., respectively. Quinelorane induced increases in 3-methoxy-4-hydroxyphenylglycol-sulfate levels in the brain stem (MED, 30 micrograms/kg i.p.) and decreases in hypothalamic epinephrine levels (MED, 100 micrograms/kg i.p.) in male rats as determined by high-pressure liquid chromatography with electrochemical detection methods. Quinelorane induced increases in extracellular ascorbic acid as determined by in vivo voltammetry in the nucleus accumbens and striatum of male rats. Quinelorane produced concentration-dependent suppression of K+-evoked release of acetylcholine from superfused caudate slices, with an IC50 of approximately 10(-8)M. Quinelorane administration produced dose-related increases in compulsive, contralateral turning in male rats with unilateral nigrostriatal lesions and increases in locomotor activity and stereotypic behavior in male rats.
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CAS 97548-97-5 Quinelorane hydrochloride

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