(R)-8-(3-Amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3

Linagliptin Linagliptin, e entsoeng ke Boehringer Ingelheim, e amohetsoe ke FDA ka la 2 Motšeanong 2011. E sebelisoa ho kopanya lijo le boikoetliso ho ntlafatsa taolo ea maemo a tsoekere ea mali ho batho ba nang le lefu la tsoekere la mofuta oa 2.Linagliptin e ntlafatsa taolo ea tsoekere ea mali ho bakuli ka ho thibela dipeptidyl peptidase-4 (DPP-4).

Incretin (Incretin) e na le phello ea ho khothaletsa tlhahiso ea insulin ke lisele tsa pancreatic islet B, haholo-holo ho kenyelletsa insulinotropic polypeptide (GIP) e itšetlehileng ka tsoekere le glucagon-like polypeptide-1 (GLP-1).DDP-4 ke serine protease e fumanehang ka holim'a lisele.E tlama liprotheine 'me e fumaneha ka bongata ho plasma le lisele tse fapaneng tsa' mele (tse kang liphio, sebete, intestinal villi e nyenyane, lisele tsa endothelial, joalo-joalo).Linagliptin ke inhibitor e ikhethileng ea DPP-4 e thibelang ts'ebetso ea enzyme ka ho tlama DPP-4, e liehisa ho senyeha ha GLP-1, e ntlafatsa ts'ebetso ea GLP-1, 'me e susumetsa ka tsela e itšetlehileng ka tsoekere ea insulin, e fokotsa boemo ba glucagon, ka hona e laola boemo ba tsoekere ea mali ho bakuli ba nang le lefu la tsoekere la mofuta oa 2.

Ha ho bapisoa le li-inhibitors tse ling tsa DPP-4, melemo ea mantlha ea Linagliptin ke: e na le polokeho e ntle ea renal mme e khona ho fokotsa hemoglobin ea glycosylated.Linagliptin e ntšoa haholo mantleng ka mokhoa oa prototype.Kamora ho tsamaisoa ka molomo, ho ntšoa ha renal ke 5% feela ea chelete e laoloang.Leha e ka tsamaisoa ka methapo, ke 30.8% feela e ntšoang ka liphio.Ka hona, ha ho hlokahale hore bakuli ba ntseng ba phekoloa.Kamehla hlahloba tšebetso ea sebete le liphio le tokiso ea lethal dose.Bakuli bohle ba ka lokisa lethal dose ka mokhoa o ts'oanang bakeng sa lengolo la ngaka le bonolo.
Litlamorao tse mpe tse tloaelehileng tsa Linagliptin ke ts'oaetso ea phefumoloho, ho tsubella nko, bohloko ba mesifa, hlooho e bohloko le 'metso.