(R)-Apomorphine Hydrochloride Hemihydrate - CAS 41372-20-7
Catalog number: 41372-20-7
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C17H18ClNO2
Molecular Weight:
303.78
COA:
Inquire
Targets:
Dopamine Receptor
Description:
(R)-Apomorphine is a non-selective dopamine agonist which activates both D1-likeand D2-like receptors, with some preference for the latter subtypes.
Purity:
≥98%
Appearance:
White Solid
Synonyms:
Apomorphine hydrochloride hemihydrate; (6aR)-5,6,6a,7-Tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol Hydrochloride Hemihydrate; 6aβ-Aporphine-10,11-diol Hydrochloride Hemihydrate;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
A non-selective dopamine agonist
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
Melting Point:
>187 °C
InChIKey:
CXWQXGNFZLHLHQ-MLVRHCEQSA-N
InChI:
1S/2C17H17NO2.2ClH.H2O/c2*1-18-8-7-10-3-2-4-12-15(10)13(18)9-11-5-6-14(19)17(20)16(11)12;;;/h2*2-6,13,19-20H,7-9H2,1H3;2*1H;1H2/t2*13-;;;/m00.../s1
Canonical SMILES:
CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O.CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O.O.Cl.Cl
Current Developer:
NeuroDerm
1.Suncus murinus: a new experimental model in emesis research.
Ueno S;Matsuki N;Saito H Life Sci. 1987 Jul 27;41(4):513-8.
Effects of various emetic and antiemetic drugs were studied using Suncus murinus for its potential use as an experimental model in emetic research. Subcutaneous injection of nicotine bitartrate (10-15 mg/kg), veratrine sulfate (0.5-1.0 mg/kg), emetine dihydrochloride (40-80 mg/kg) and oral administration of copper sulfate (20-100 mg/kg) caused dose-dependent emesis in suncus. The ED50 of nicotine, veratrine, emetine and copper sulfate were 7.9, 0.4, 47.6 and 21.4 mg/kg, respectively. However, subcutaneously injected apomorphine hydrochloride (0.1-100 mg/kg), digitoxin (0.5-1.0 mg/kg) and orally administered emetine dihydrochloride (10-80 mg/kg) did not induce the vomiting. Chlorpromazine and promethazine decreased the emetic effect of nicotine, veratrine and copper sulfate, but scopolamine hydrobromide was not effective. These results indicate that the Suncus murinus is sensitive to various emetic and antiemetic drugs and can be used as a new experimental animal model for the emesis. Emetic behavior of suncus was discussed in comparison with other animals.
2.MK-801 increases locomotor activity without elevating extracellular dopamine levels in the nucleus accumbens.
Druhan JP;Rajabi H;Stewart J Synapse. 1996 Oct;24(2):135-46.
In vivo microdialysis was used in freely moving rats to determine whether the locomotor stimulant effects of dizocilpine maleate (MK-801) were related to increased dopamine (DA) release within the nucleus accumbens (N. Acc.). Each experiment began with a baseline period of at least 2 h (starting 15-20 h after insertion of concentric, removable dialysis probes), during with activity records and dialysate samples were collected every 20 min. Rats in the first experiment then were injected with MK-801 (0.125, 0.25, or 0.50 mg/kg, i.p.) or saline, and activity and extracellular levels of DA, dihydroxyphenylacetic acid (DOPAC), and homovanillic acid (HVA) were measured for a further 160 min post-injection. In a second experiment, rats were given 1.5 mg/kg d-amphetamine sulphate 40 min after receiving the same doses of MK-801, and testing was continued for 120 min. Rats in a third experiment were given low, autoreceptor-preferring doses of apomorphine hydrochloride (25 or 50 micrograms/kg, s.c.) or its vehicle 40 min after injection of 0.25 mg/kg MK-801 and then monitored for 120 min. MK-801 produced strong and consistent increases in locomotor activity that were augmented by amphetamine and greatly reduced by the low doses of apomorphine.
3.An open-label, randomized, flexible-dose, crossover study to assess the comparative efficacy and safety of sildenafil citrate and apomorphine hydrochloride in men with erectile dysfunction.
Giammusso B;Colpi GM;Cormio L;Ludovico G;Soli M;Ponchietti R;Montorsi F;Panzironi C;Guastella B Urol Int. 2008;81(4):409-15. doi: 10.1159/000167838. Epub 2008 Dec 10.
INTRODUCTION: ;We report the methodology and results of a study that compared a dopaminergic agonist, apomorphine, with a phosphodiesterase type-5 inhibitor, sildenafil, in terms of efficacy, tolerability, satisfaction and patient preference.;PATIENTS AND METHODS: ;This was a 20-week open- label, randomized, flexible-dose, crossover study to assess the comparative efficacy and safety of sildenafil and apomorphine. One sequence group received treatment with sildenafil followed by apomorphine and the other sequence group received treatment with apomorphine followed by sildenafil. The primary efficacy variable was the measurement of the score of the erectile function domain (the sum of questions 1-5 and 15) of the International Index of Erectile Function (IIEF) questionnaire. The secondary efficacy variables were: the responses to the Global Efficacy Assessment Questions; the score of the responses to all the questions of the IIEF questionnaire; the index score of the Erectile Dysfunction Inventory of Treatment Satisfaction questionnaire, and the event log variables.;RESULTS AND CONCLUSIONS: ;A marked increase in the mean IIEF score was observed after treatment with sildenafil, compared with a small increase following treatment with apomorphine.
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CAS 41372-20-7 (R)-Apomorphine Hydrochloride Hemihydrate

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