Tìm theo
Terlipressin
Các tên gọi khác (5 ) :
  • SID124896640
  • Terlipressin
  • Terlipressina
  • Terlipressine
  • Terlipressinum
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 14636-12-5
ATC: H01BA04
CTHH: C52H74N16O15S2
PTK: 1227.372
Terlipressin is an analogue of vasopressin used as a vasoactive drug in the management of hypotension. It has been found to be effective when norepinephrine does not help. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C52H74N16O15S2
Phân tử khối
1227.372
Monoisotopic mass
1226.496097158
InChI
InChI=1S/C52H74N16O15S2/c53-17-5-4-9-31(45(76)60-23-41(57)72)63-51(82)38-10-6-18-68(38)52(83)37-27-85-84-26-36(61-44(75)25-59-43(74)24-58-42(73)22-54)50(81)65-34(20-29-11-13-30(69)14-12-29)48(79)64-33(19-28-7-2-1-3-8-28)47(78)62-32(15-16-39(55)70)46(77)66-35(21-40(56)71)49(80)67-37/h1-3,7-8,11-14,31-38,69H,4-6,9-10,15-27,53-54H2,(H2,55,70)(H2,56,71)(H2,57,72)(H,58,73)(H,59,74)(H,60,76)(H,61,75)(H,62,78)(H,63,82)(H,64,79)(H,65,81)(H,66,77)(H,67,80)/t31-,32-,33-,34-,35-,36-,37-,38-/m0/s1
InChI Key
InChIKey=BENFXAYNYRLAIU-QSVFAHTRSA-N
IUPAC Name
(2S)-6-amino-2-{[(2S)-1-{[(4R,7S,10S,13S,16S,19R)-19-{2-[2-(2-aminoacetamido)acetamido]acetamido}-13-benzyl-10-(2-carbamoylethyl)-7-(carbamoylmethyl)-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-4-yl]carbonyl}pyrrolidin-2-yl]formamido}-N-(carbamoylmethyl)hexanamide
Traditional IUPAC Name
terlipressin
SMILES
NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)CNC(=O)CNC(=O)CN)C(=O)N[C@@H](CC2=CC=C(O)C=C2)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
Độ hòa tan
1.67e-01 g/l
logP
-10
logS
-3.9
pKa (strongest acidic)
9.43
pKa (Strongest Basic)
10.26
PSA
512.85 Å2
Refractivity
305.18 m3·mol-1
Polarizability
123.88 Å3
Rotatable Bond Count
25
H Bond Acceptor Count
17
H Bond Donor Count
16
Physiological Charge
2
Number of Rings
4
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Terlipressin is a medicine similar to a naturally occurring hormone present in the body, known as antidiuretic hormone (ADH) or vasopressin. ADH has two main effects in the body. Firstly, it causes narrowing of blood vessels (vasoconstriction), thereby limiting blood flow to a particular area of the body. It also acts on receptors in the kidney to retain water in the body, which helps to prevent excessive loss of water in the urine.
Cơ Chế Tác Dụng : Terlipressin is an analogue of vasopressin used as a vasoactive drug in the management of hypotension. It has been found to be effective when norepinephrine does not help. [Wikipedia] Terlipressin, an analogue of vasopressin, acts on three different receptors, vasopressin receptor V1a (which initiates vasoconstriction, liver gluconeogenesis, platelet aggregation and release of factor VIII), vasopressin receptor V1b (which mediates corticotrophin secretion from the pituitary) and vasopressin receptor V2 which controls free water reabsorption in the renal medullar. The binding of terlipressin to the V2 receptor activates adenylate cyclase which causes the release of aquaporin 2 channels into the cells lining the renal medullar duct. This allows water to be reabsorbed down an osmotic gradient so the urine is more concentrated.
Dược Động Học :

▧ Protein binding :
Approximately 30%
Chỉ Định : Commonly used to stop bleeding of varices in the food pipe (oesophagus).
Liều Lượng & Cách Dùng : Injection, solution - Intravenous
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB02638
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=72081
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504626
ChemSpider
http://www.chemspider.com/Chemical-Structure.65067.html
PharmGKB
http://www.pharmgkb.org/drug/PA164781020
Wikipedia
http://en.wikipedia.org/wiki/Terlipressin
... loading
... loading