| 词条 | JTC-801 |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 444655127 | IUPAC_name = N-(4-amino-2-methylquinolin-6-yl)-2-[(4-ethylphenoxy)methyl]benzamide | image = JTC-801.png | width = 200 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 244218-51-7 | ATC_prefix = | ATC_suffix = | IUPHAR_ligand = 1692 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | PubChem = 5311340 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 4470841 | smiles = O=C(c1ccccc1COc2ccc(cc2)CC)Nc3ccc4nc(cc(c4c3)N)C | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C26H25N3O2/c1-3-18-8-11-21(12-9-18)31-16-19-6-4-5-7-22(19)26(30)29-20-10-13-25-23(15-20)24(27)14-17(2)28-25/h4-15H,3,16H2,1-2H3,(H2,27,28)(H,29,30) | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = VTGBZWHPJFMTKS-UHFFFAOYSA-N | C=26 | H=25 | N=3 | O=2 | molecular_weight = 411.51 g/mol | synonyms = JTC-801 }}JTC-801 is an opioid analgesic drug used in scientific research.[1][2] JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor.[3] This was the fourth opioid receptor to be discovered and is still the least understood. The nociceptin receptor has complex effects which are involved in many processes involved in pain and inflammation responses, and activation of this receptor can either increase or reduce pain depending on dose.[4] Drugs acting at the noiciceptin receptor may influence the effects of traditional analgesics such as NSAIDs,[5] μ-opioid agonists,[6] and cannabinoids.[7] JTC-801 is an orally active drug that blocks the nociceptin receptor and produces analgesic effects in a variety of animal studies, and is particularly useful for neuropathic pain and allodynia associated with nerve injury.[8][9][10] See also
References1. ^{{cite journal | last1 = Shinkai | first1 = H | last2 = Ito | first2 = T | last3 = Iida | first3 = T | last4 = Kitao | first4 = Y | last5 = Yamada | first5 = H | last6 = Uchida | first6 = I | title = 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity | journal = Journal of Medicinal Chemistry | volume = 43 | issue = 24 | pages = 4667–77 | year = 2000 | pmid = 11101358 |name-list-format=vanc | doi=10.1021/jm0002073}} {{Opioidergics}}{{analgesic-stub}}2. ^{{cite journal | last1 = Yamada | first1 = H | last2 = Nakamoto | first2 = H | last3 = Suzuki | first3 = Y | last4 = Ito | first4 = T | last5 = Aisaka | first5 = K | title = Pharmacological profiles of a novel opioid receptor-like1 (ORL1) receptor antagonist, JTC-801 | journal = British Journal of Pharmacology | volume = 135 | issue = 2 | pages = 323–32 | year = 2002 | pmid = 11815367 |name-list-format=vanc | pmc = 1573142 | doi = 10.1038/sj.bjp.0704478 }} 3. ^{{cite journal | last1 = Sestili | first1 = I | last2 = Borioni | first2 = A | last3 = Mustazza | first3 = C | last4 = Rodomonte | first4 = A | last5 = Turchetto | first5 = L | last6 = Sbraccia | first6 = M | last7 = Riitano | first7 = D | last8 = Del Giudice | first8 = MR | title = A new synthetic approach of N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide (JTC-801) and its analogues and their pharmacological evaluation as nociceptin receptor (NOP) antagonists | journal = European Journal of Medicinal Chemistry | volume = 39 | issue = 12 | pages = 1047–57 | year = 2004 | pmid = 15571866 |name-list-format=vanc | doi = 10.1016/j.ejmech.2004.09.009 }} 4. ^{{cite journal | last1 = Muratani | first1 = T | last2 = Minami | first2 = T | last3 = Enomoto | first3 = U | last4 = Sakai | first4 = M | last5 = Okuda-Ashitaka | first5 = E | last6 = Kiyokane | first6 = K | last7 = Mori | first7 = H | last8 = Ito | first8 = S | title = Characterization of nociceptin/orphanin FQ-induced pain responses by the novel receptor antagonist N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl) benzamide monohydrochloride | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 303 | issue = 1 | pages = 424–30 | year = 2002 | pmid = 12235279 |name-list-format=vanc | doi = 10.1124/jpet.102.036095 }} 5. ^{{cite journal | last1 = Okuda-Ashitaka | first1 = E | last2 = Minami | first2 = T | last3 = Matsumura | first3 = S | last4 = Takeshima | first4 = H | last5 = Reinscheid | first5 = RK | last6 = Civelli | first6 = O | last7 = Ito | first7 = S | title = The opioid peptide nociceptin/orphanin FQ mediates prostaglandin E2-induced allodynia, tactile pain associated with nerve injury | journal = The European Journal of Neuroscience | volume = 23 | issue = 4 | pages = 995–1004 | year = 2006 | pmid = 16519664 |name-list-format=vanc | doi = 10.1111/j.1460-9568.2006.04623.x }} 6. ^{{cite journal | last1 = Zaveri | first1 = N | last2 = Jiang | first2 = F | last3 = Olsen | first3 = C | last4 = Polgar | first4 = W | last5 = Toll | first5 = L | title = Small-molecule agonists and antagonists of the opioid receptor-like receptor (ORL1, NOP): Ligand-based analysis of structural factors influencing intrinsic activity at NOP | journal = The AAPS Journal | volume = 7 | issue = 2 | pages = E345–52 | year = 2005 | pmid = 16353914 |name-list-format=vanc | pmc = 2750971 | doi = 10.1208/aapsj070234 }} 7. ^{{cite journal | last1 = Rawls | first1 = SM | last2 = Schroeder | first2 = JA | last3 = Ding | first3 = Z | last4 = Rodriguez | first4 = T | last5 = Zaveri | first5 = N | title = NOP receptor antagonist, JTC-801, blocks cannabinoid-evoked hypothermia in rats | journal = Neuropeptides | volume = 41 | issue = 4 | pages = 239–47 | year = 2007 | pmid = 17512052 |name-list-format=vanc | doi = 10.1016/j.npep.2007.03.001 }} 8. ^{{cite journal | last1 = Mabuchi | first1 = T | last2 = Matsumura | first2 = S | last3 = Okuda-Ashitaka | first3 = E | last4 = Kitano | first4 = T | last5 = Kojima | first5 = H | last6 = Nagano | first6 = T | last7 = Minami | first7 = T | last8 = Ito | first8 = S | title = Attenuation of neuropathic pain by the nociceptin/orphanin FQ antagonist JTC-801 is mediated by inhibition of nitric oxide production | journal = The European Journal of Neuroscience | volume = 17 | issue = 7 | pages = 1384–92 | year = 2003 | pmid = 12713641 |name-list-format=vanc | doi = 10.1046/j.1460-9568.2003.02575.x }} 9. ^{{cite journal | last1 = Suyama | first1 = H | last2 = Kawamoto | first2 = M | last3 = Gaus | first3 = S | last4 = Yuge | first4 = O | title = Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model | journal = Neuroscience Letters | volume = 351 | issue = 3 | pages = 133–6 | year = 2003 | pmid = 14623124 |name-list-format=vanc | doi=10.1016/S0304-3940(03)00502-0}} 10. ^{{cite journal | last1 = Tamai | first1 = H | last2 = Sawamura | first2 = S | last3 = Takeda | first3 = K | last4 = Orii | first4 = R | last5 = Hanaoka | first5 = K | title = Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation | journal = European Journal of Pharmacology | volume = 510 | issue = 3 | pages = 223–8 | year = 2005 | pmid = 15763246 |name-list-format=vanc | doi = 10.1016/j.ejphar.2005.01.033 }} 6 : Synthetic opioids|Quinolines|Benzamides|Aromatic amines|Phenol ethers|Nociceptin receptor antagonists |
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