| 词条 | Vedaclidine |
| 释义 |
| IUPAC_name = (3S)-3-[4-(Butylsulfanyl)-1,2,5-thiadiazol-3-yl]quinuclidine | image = Vedaclidine.svg | width = 175 | tradename = | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number = 141575-52-2 | ATC_prefix = None | ATC_suffix = | PubChem = 9889093 | ChemSpiderID = 8064764 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 98IW5HAV1N | ChEMBL = 136807 | C=13 | H=21 | N=3 | S=2 | molecular_weight = 283.455 g/mol | SMILES = CCCCSC1=NSN=C1[C@@H]2CN3CCC2CC3 | StdInChI = 1S/C13H21N3S2/c1-2-3-8-17-13-12(14-18-15-13)11-9-16-6-4-10(11)5-7-16/h10-11H,2-9H2,1H3/t11-/m1/s1 | StdInChIKey = WZZPXVURFDJHGI-LLVKDONJSA-N | synonyms = (S)-3-[4-(butylthio)-1,2,5-thiadiazol-3-yl]quinuclidine }}Vedaclidine (INN,[1]{{rp|180}} codenamed LY-297,802, NNC 11-1053) is a novel analgesic drug which acts as a mixed agonist–antagonist at muscarinic acetylcholine receptors, being a potent and selective agonist for the M1 and M4 subtypes, yet an antagonist at the M2, M3 and M5 subtypes.[2][3] It is orally active and an effective analgesic over 3× the potency of morphine, with side effects such as salivation and tremor only occurring at many times the effective analgesic dose.[4][5][6] Human trials showed little potential for development of dependence or abuse,[7] and research is continuing into possible clinical application in the treatment of neuropathic pain and cancer pain relief.[8] See also
References1. ^{{cite web | title = International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names (Rec. INN): List 38 | url = http://www.who.int/medicines/publications/druginformation/innlists/RL38.pdf | publisher = World Health Organization | accessdate = 18 November 2016 | date = 1997}} {{Analgesics}}{{Muscarinic acetylcholine receptor modulators}}2. ^{{cite journal | last1 = Shannon | first1 = HE | last2 = Womer | first2 = DE | last3 = Bymaster | first3 = FP | last4 = Calligaro | first4 = DO | last5 = DeLapp | first5 = NC | last6 = Mitch | first6 = CH | last7 = Ward | first7 = JS | last8 = Whitesitt | first8 = CA | last9 = Swedberg | first9 = MD | last10 = Sheardown | first10 = M. J. | last11 = Fink-Jensen | first11 = A | last12 = Olesen | first12 = P. H. | last13 = Rimvall | first13 = K | last14 = Sauerberg | first14 = P | year = 1997 | title = In vivo pharmacology of butylthio[2.2.2] (LY297802 / NNC11-1053), an orally acting antinociceptive muscarinic agonist | url = | journal = Life Sciences | volume = 60 | issue = 13–14| pages = 969–76 | pmid = 9121363 | display-authors = 3 | doi=10.1016/s0024-3205(97)00036-2}} 3. ^{{cite journal | last1 = Womer | first1 = DE | last2 = Shannon | first2 = HE | title = Reversal of pertussis toxin-induced thermal allodynia by muscarinic cholinergic agonists in mice | journal = Neuropharmacology | volume = 39 | issue = 12 | pages = 2499–504 | year = 2000 | pmid = 10974334 | doi=10.1016/S0028-3908(00)00068-X}} 4. ^{{cite journal | last1 = Swedberg | first1 = MD | last2 = Sheardown | first2 = MJ | last3 = Sauerberg | first3 = P | last4 = Olesen | first4 = PH | last5 = Suzdak | first5 = PD | last6 = Hansen | first6 = KT | last7 = Bymaster | first7 = FP | last8 = Ward | first8 = JS | last9 = Mitch | first9 = CH | last10 = Calligaro | first10 = D. O. | last11 = Delapp | first11 = N. W. | last12 = Shannon | first12 = H. E. |date=May 1997 | title = Butylthio[2.2.2] (NNC 11-1053/LY297802) an orally active muscarinic agonist analgesic | url = | journal = Journal of Pharmacology and Experimental Therapeutics | volume = 281 | issue = 2| pages = 876–83 | pmid = 9152397 | display-authors = 3 }} 5. ^{{cite journal | last1 = Shannon | first1 = HE | last2 = Sheardown | first2 = MJ | last3 = Bymaster | first3 = FP | last4 = Calligaro | first4 = DO | last5 = Delapp | first5 = NW | last6 = Gidda | first6 = J | last7 = Mitch | first7 = CH | last8 = Sawyer | first8 = BD | last9 = Stengel | first9 = PW | last10 = Ward | first10 = J. S. | last11 = Wong | first11 = D. T. | last12 = Olesen | first12 = P. H. | last13 = Suzdak | first13 = P. D. | last14 = Sauerberg | first14 = P | last15 = Swedberg | first15 = M. D. |date=May 1997 | title = Pharmacology of butylthio[2.2.2] (LY297802/NNC11-1053) a novel analgesic with mixed muscarinic receptor agonist and antagonist activity | url = | journal = Journal of Pharmacology and Experimental Therapeutics | volume = 281 | issue = 2| pages = 884–94 | pmid = 9152398 | display-authors = 3 }} 6. ^{{cite journal | last1 = Shannon | first1 = HE | last2 = Jones | first2 = CK | last3 = Li | first3 = DL | last4 = Peters | first4 = SC | last5 = Simmons | first5 = RM | last6 = Iyengar | first6 = S | title = Antihyperalgesic effects of the muscarinic receptor ligand vedaclidine in models involving central sensitization in rats | journal = Pain | volume = 93 | issue = 3 | pages = 221–7 | year = 2001 | pmid = 11514081 | doi=10.1016/S0304-3959(01)00319-0}} 7. ^{{cite journal | last1 = Petry | first1 = NM | last2 = Bickel | first2 = WK | last3 = Huddleston | first3 = J | last4 = Tzanis | first4 = E | last5 = Badger | first5 = GJ | title = A comparison of subjective, psychomotor and physiological effects of a novel muscarinic analgesic, LY297802 tartrate, and oral morphine in occasional drug users | journal = Drug and Alcohol Dependence | volume = 50 | issue = 2 | pages = 129–36 | year = 1998 | pmid = 9649964 | doi=10.1016/S0376-8716(98)00026-X}} 8. ^{{cite journal | last1 = Tata | first1 = AM | title = Muscarinic acetylcholine receptors: new potential therapeutic targets in antinociception and in cancer therapy | journal = Recent patents on CNS drug discovery | volume = 3 | issue = 2 | pages = 94–103 | year = 2008 | pmid = 18537768 | doi = 10.2174/157488908784534621 }} 6 : Analgesics|Muscarinic agonists|Muscarinic antagonists|Quinuclidines|Thiadiazoles|Thioethers |
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