| 词条 | Zacopride |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 396760537 | IUPAC_name = 4-amino-5-chloro-2-methoxy-N-(quinuclidin-3-yl)benzamide | image = Zacopride.svg | width = 220 | tradename = | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 90182-92-6 | ATC_prefix = none | ATC_suffix = | PubChem = 108182 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 97262 | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C15H20ClN3O2/c1-21-14-7-12(17)11(16)6-10(14)15(20)18-13-8-19-4-2-9(13)3-5-19/h6-7,9,13H,2-5,8,17H2,1H3,(H,18,20) | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = FEROPKNOYKURCJ-UHFFFAOYSA-N | IUPHAR_ligand = 245 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | UNII_Ref = {{fdacite|changed|FDA}} | UNII = 9GN3OT4156 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 18041 | C=15 | H=20 | Cl=1 | N=3 | O=2 | molecular_weight = 309.791 g/mol | smiles = COC1=CC(=C(C=C1C(=O)NC2CN3CCC2CC3)Cl)N }}Zacoprideis a potent antagonist at the 5-HT3 receptor[1] and an agonist at the 5-HT4 receptor.[2] It has anxiolytic[3] and nootropic effects in animal models,[4] with the (R)-(+)-enantiomer being the more active form.[5] It also has antiemetic[6] and pro-respiratory effects, both reducing sleep apnea[7] and reversing opioid-induced respiratory depression in animal studies.[8] Early animal trials have also revealed that administration of zacopride can reduce preference for and consumption of ethanol.[9] Zacopride was found to significantly increase aldosterone levels in human subjects for 180 minutes at a dose of 400 micrograms. It is thought to do this by stimulating the 5-HT4 receptors on the adrenal glands. Zacopride also stimulated aldosterone secretion when applied to human adrenal glands in vitro. No significant changes were observed in renin, ACTH, or cortisol levels.[2] Zacopride has been tested in clinical trials for the treatment of schizophrenia, but was found unsuccessful.[10] References1. ^{{cite journal | last1 = Smith | first1 = WW | last2 = Sancilio | first2 = LF | last3 = Owera-Atepo | first3 = JB | last4 = Naylor | first4 = RJ | last5 = Lambert | first5 = L | title = Zacopride, a potent 5-HT3 antagonist | journal = The Journal of Pharmacy and Pharmacology | volume = 40 | issue = 4 | pages = 301–2 | year = 1988 | pmid = 2900319 | doi = 10.1111/j.2042-7158.1988.tb05253.x }} {{Other respiratory system products}}{{Serotonergics}}{{nervous-system-drug-stub}}{{respiratory-system-drug-stub}}2. ^1 {{cite journal | last1 = Lefebvre | first1 = H | last2 = Contesse | first2 = V | last3 = Delarue | first3 = C | last4 = Soubrane | first4 = C | last5 = Legrand | first5 = A | last6 = Kuhn | first6 = JM | last7 = Wolf | first7 = LM | last8 = Vaudry | first8 = H | title = Effect of the serotonin-4 receptor agonist zacopride on aldosterone secretion from the human adrenal cortex: in vivo and in vitro studies | journal = The Journal of Clinical Endocrinology and Metabolism | volume = 77 | issue = 6 | pages = 1662–6 | year = 1993 | pmid = 8263156 | doi=10.1210/jc.77.6.1662}} 3. ^{{cite journal | last1 = Costall | first1 = B | last2 = Domeney | first2 = AM | last3 = Gerrard | first3 = PA | last4 = Kelly | first4 = ME | last5 = Naylor | first5 = RJ | title = Zacopride: anxiolytic profile in rodent and primate models of anxiety | journal = The Journal of Pharmacy and Pharmacology | volume = 40 | issue = 4 | pages = 302–5 | year = 1988 | pmid = 2900320 | doi = 10.1111/j.2042-7158.1988.tb05254.x }} 4. ^{{cite journal | last1 = Fontana | first1 = DJ | last2 = Daniels | first2 = SE | last3 = Eglen | first3 = RM | last4 = Wong | first4 = EH | title = Stereoselective effects of (R)- and (S)-zacopride on cognitive performance in a spatial navigation task in rats | journal = Neuropharmacology | volume = 35 | issue = 3 | pages = 321–7 | year = 1996 | pmid = 8783207 | doi=10.1016/0028-3908(96)00191-8}} 5. ^{{cite journal | last1 = Young | first1 = R | last2 = Johnson | first2 = DN | title = Anxiolytic-like activity of R(+)- and S(−)-zacopride in mice | journal = European Journal of Pharmacology | volume = 201 | issue = 2–3 | pages = 151–5 | year = 1991 | pmid = 1686755 | doi=10.1016/0014-2999(91)90338-Q}} 6. ^{{cite journal | last1 = Yamakuni | first1 = H | last2 = Nakayama | first2 = H | last3 = Matsui | first3 = S | last4 = Imazumi | first4 = K | last5 = Matsuo | first5 = M | last6 = Mutoh | first6 = S | title = Inhibitory effect of zacopride on Cisplatin-induced delayed emesis in ferrets | journal = Journal of pharmacological sciences | volume = 101 | issue = 1 | pages = 99–102 | year = 2006 | pmid = 16651699 | doi = 10.1254/jphs.SCJ05007X }} 7. ^{{cite journal | last1 = Carley | first1 = DW | last2 = Depoortere | first2 = H | last3 = Radulovacki | first3 = M | title = R-zacopride, a 5-HT3 antagonist/5-HT4 agonist, reduces sleep apneas in rats | journal = Pharmacology Biochemistry and Behavior | volume = 69 | issue = 1–2 | pages = 283–9 | year = 2001 | pmid = 11420096 | doi=10.1016/S0091-3057(01)00535-4}} 8. ^{{cite journal | last1 = Meyer | first1 = LC | last2 = Fuller | first2 = A | last3 = Mitchell | first3 = D | title = Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats | journal = American Journal of Physiology. Regulatory, Integrative and Comparative Physiology | volume = 290 | issue = 2 | pages = R405–13 | year = 2006 | pmid = 16166206 | doi = 10.1152/ajpregu.00440.2005 }} 9. ^{{cite journal|last1=Knapp|first1=D.J.|last2=Pohorecky|first2=L.A.|title=Zacopride, a 5-HT3 receptor antagonist, reduces voluntary ethanol consumption in rats|journal=Pharmacology Biochemistry and Behavior|volume=41|issue=4|year=1992|pages=847–850|issn=0091-3057|doi=10.1016/0091-3057(92)90237-A}} 10. ^{{cite journal|last1=Faustman|first1=William O.|title=Zacopride in Schizophrenia: A Single-blind Serotonin Type 3 Antagonist Trial|journal=Archives of General Psychiatry|volume=49|issue=9|year=1992|pages=751|issn=0003-990X|doi=10.1001/archpsyc.1992.01820090079013}} 8 : 5-HT3 antagonists|Anilines|Benzamides|Chloroarenes|Phenol ethers|Quinuclidines|Respiratory agents|Serotonin receptor agonists |
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