| 词条 | Mavatrep |
| 释义 |
| drug_name = | INN = | type = | IUPAC_name = 2-[2-[2-[(E)-2-[4-(Trifluoromethyl)phenyl]ethenyl]-3H-benzimidazol-5-yl]phenyl]propan-2-ol | image = Mavatrep.svg | caption = | pronounce = | tradename = | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_AU_comment = | pregnancy_US = | pregnancy_category= | routes_of_administration = | legal_AU = | legal_AU_comment = | legal_BR = | legal_BR_comment = | legal_CA = | legal_DE = | legal_NZ = | legal_UK = | legal_US = | legal_UN = | legal_status = | bioavailability = | protein_bound = | metabolism = | metabolites = | onset = | elimination_half-life = | duration_of_action = | excretion = | CAS_number = 956274-94-5 | class = | ATCvet = | ATC_prefix = | ATC_suffix = | PubChem = 17751090 | ChemSpiderID = 29271895 | DrugBank = DB12875 | UNII = F197218T99 | ChEMBL = 2364618 | synonyms = JNJ-39439335 | C=25|H=21|F=3|N=2|O=1 | StdInChI=1S/C25H21F3N2O/c1-24(2,31)20-6-4-3-5-19(20)17-10-13-21-22(15-17)30-23(29-21)14-9-16-7-11-18(12-8-16)25(26,27)28/h3-15,31H,1-2H3,(H,29,30)/b14-9+ | StdInChIKey = ORDHXXHTBUZRCN-NTEUORMPSA-N | smiles = CC(C)(C1=CC=CC=C1C2=CC3=C(C=C2)N=C(N3)/C=C/C4=CC=C(C=C4)C(F)(F)F)O }} Mavatrep (JNJ‐39439335) is a TRPV1 receptor selective competitive antagonist.[1] It is an investigational analgesic that may be a potential treatment for analgesia and/or inflammation. Phase I trials have been completed in healthy Japanese and Caucasian volunteers.[1][2] Potential common adverse effects include thermohypoesthesia, chills, feeling cold, and feeling hot.[2] PharmacokineticsWhen administered orally once a day, mavatrep reached steady-state in healthy volunteers in approximately 14 days.[2] It has a relatively long half life between 68–101 hours in Japanese subjects and between 82–130 hours in Caucasian subjects.[2] Mavatrep is largely eliminated nonrenally. Mavatrep appears to be metabolized into two primary metabolites which are also eliminated nonrenally.[2] References1. ^1 {{Cite journal|last=Manitpisitkul|first=Prasarn|last2=Shalayda|first2=Kevin|last3=Russell|first3=Lucille|last4=Sanga|first4=Panna|last5=Williams|first5=Yinka|last6=Solanki|first6=Bhavna|last7=Caruso|first7=Joseph|last8=Moyer|first8=John A.|date=2018|title=Bioavailability and Pharmacokinetics of TRPV1 Antagonist Mavatrep (JNJ-39439335) Tablet and Capsule Formulations in Healthy Men: Two Open-Label, Crossover, Single-Dose Phase 1 Studies|url=https://accp1.onlinelibrary.wiley.com/doi/abs/10.1002/cpdd.412|journal=Clinical Pharmacology in Drug Development|language=en|volume=7|issue=7|pages=699–711|doi=10.1002/cpdd.412|issn=2160-7648}} 2. ^1 2 3 4 {{Cite journal|last=Manitpisitkul|first=Prasarn|last2=Shalayda|first2=Kevin|last3=Russell|first3=Lucille|last4=Sanga|first4=Panna|last5=Solanki|first5=Bhavna|last6=Caruso|first6=Joseph|last7=Iwaki|first7=Yuki|last8=Moyer|first8=John A.|date=2018|title=Pharmacokinetics and Safety of Mavatrep (JNJ-39439335), a TRPV1 Antagonist in Healthy Japanese and Caucasian Men: A Double-Blind, Randomized, Placebo-Controlled, Sequential-Group Phase 1 Study|url=https://accp1.onlinelibrary.wiley.com/doi/abs/10.1002/cpdd.413|journal=Clinical Pharmacology in Drug Development|language=en|volume=7|issue=7|pages=712–726|doi=10.1002/cpdd.413|issn=2160-7648}} 3 : Ion channel blockers|Analgesics|Experimental drugs |
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