(-)-Quinpirole hydrochloride - CAS 85798-08-9
Category: Inhibitor
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Molecular Formula:
C13H21N3.HCl
Molecular Weight:
255.79
COA:
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Targets:
Dopamine Receptor
Description:
(-)-Quinpirole hydrochloride is a selective dopamine D2 receptor agonist, with high affinity for the D2 and D3 dopamine receptor subtypes (Ki values are 4.8, ~24, ~30 and 1900 nM at D2, D3, D4 and D1 receptors respectively).
Purity:
≥98% by HPLC
Synonyms:
(4aR-trans)-4,4a,5,6,7,8,8a,9-Octahydro-5-propyl-1H-pyrazolo[3,4-g]quinoline hydrochloride; (-)-Quinpirole hydrochloride; (-)Quinpirole hydrochloride; (-)-Quinpirole HCl; (-)Quinpirole HCl; (-) Quinpirole HCl; LY-171555; LY 171555; LY171555
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
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InChIKey:
HJHVRVJTYPKTHX-HTMVYDOJSA-N
InChI:
InChI=1S/C13H21N3.ClH/c1-2-5-16-6-3-4-10-7-12-11(8-13(10)16)9-14-15-12;/h9-10,13H,2-8H2,1H3,(H,14,15);1H/t10-,13-;/m1./s1
Canonical SMILES:
CCCN1CCCC2C1CC3=C(C2)NN=C3.Cl
1.SKF 38393 potentiates yawning induced by LY 171555: further evidence against the autoreceptor hypothesis of yawning.
Spina L;Longoni R;Mulas A;Di Chiara G Psychopharmacology (Berl). 1989;98(4):567-8.
The effect of concurrent D-1 receptor stimulation by SKF 38393 on the expression of yawning elicited by D-2 receptor stimulation with LY 171555 was studied in the rat. A low dose of SKF 38393 (2.5 mg/kg SC), while failed to elicit yawning, potentiated the effectiveness of LY 171555 in eliciting yawning at all the doses tested (12.5, 25 and 50 micrograms/kg SC) and this effect was abolished by SCH 23390 (0.012 mg/kg SC). The results indicate that in analogy with typical post-synaptic dopaminergic effects (hypermotility-stereotypy), yawning elicited by a D-2 agonist is facilitated by concurrent stimulation of D-1 receptors and therefore is consistent with previous evidence that yawning in response to a D-2 agonist is not mediated by autoreceptors.
2.Yawning is elicited by D2 dopamine agonists but is blocked by the D1 antagonist, SCH 23390.
Serra G;Collu M;Gessa GL Psychopharmacology (Berl). 1987;91(3):330-3.
The subtype of dopamine (DA) receptors mediating the yawning response to DA agonists was determined in rats. Yawning was elicited both by the mixed D1-D2 agonist apomorphine and by the specific D2 agonist LY 171555, but not by the selective D1 agonist SKF 38393. Both apomorphine- and LY 171555-induced yawning were antagonized not only by the selective D2 antagonist sulpiride but, unexpectedly, also by the selective D1 antagonist SCH 23390. The results suggest that DA receptors mediating the yawning response are of the D2 type, and that these receptors are connected with D1 receptors in such a way that the blockade of the latter results in the functional inactivation of the former.
3.Potential therapeutic use of the selective dopamine D1 receptor agonist, A-86929: an acute study in parkinsonian levodopa-primed monkeys.
Grondin R;Bédard PJ;Britton DR;Shiosaki K Neurology. 1997 Aug;49(2):421-6.
The clinical utility of dopamine (DA) D1 receptor agonists in the treatment of Parkinson's disease (PD) is still unclear. The therapeutic use of selective DA D1 receptor agonists such as SKF-82958 (6-chloro-7,8-dihydroxy-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzaze pine hydrobromide) and A-77636 ([1R, 3S] 3-[1'-admantyl]-1-aminomethyl-3,4-dihydro-5,6-dihydroxy-1H-2-benzo pyran hydrochloride) seems limited because of their duration of action, which is too short for SKF-82958 (< 1 hr) and too long for A-77636 (> 20 hr, leading to behavioral tolerance). We therefore conducted the present acute dose-response study in four 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-exposed cynomolgus monkeys primed to exhibit levodopa-induced dyskinesias to evaluate the locomotor and dyskinetic effects on challenge with four doses (from 0.03 to 1.0 mg/kg) of A-86929 ([-]-[5aR,11bS]-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-+ ++azacyclopent-1- ena[c]phenathrene-9-10-diol), a selective and full DA D1-like receptor agonist with an intermediate duration of action. Levodopa and the DA D2-like receptor agonist, LY-171555 ([4aR-trans]-4,4a,5,6,7,8,8a,9-o-dihydro-5n-propyl-2H-pyrazo lo-3-4-quinoline hydrochloride) were also used for comparison.
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Chemical Structure

CAS 85798-08-9 (-)-Quinpirole hydrochloride

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