Tìm theo
Mepyramine
Các tên gọi khác (6 ) :
  • Mepyramine
  • N-(P-Methoxybenzyl)-n',n'-dimethyl-N-(alpha-pyridyl)ethylenediamine
  • N-[(4-Methoxyphenyl)methyl]-n',n'-dimethyl-N-2-pyridinyl-1,2-ethanediamine
  • N',n'-dimethyl-N-(P-methoxybenzyl)-N-(2-pyridyl)ethylenediamine
  • Pyranisamine
  • pyrilamine
Thuốc chống dị ứng
Thuốc Gốc
Small Molecule
CAS: 91-84-9
ATC: R06AC01, D04AA02
CTHH: C17H23N3O
PTK: 285.384
Mepyramine (also known as pyrilamine) is a first generation antihistamine, targeting the H1 receptor. However, it rapidly permeates the brain and so often causes drowsiness as a side effect. It is used in over-the-counter combination products for colds and menstrual symptoms.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H23N3O
Phân tử khối
285.384
Monoisotopic mass
285.184112373
InChI
InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3
InChI Key
InChIKey=YECBIJXISLIIDS-UHFFFAOYSA-N
IUPAC Name
N-[2-(dimethylamino)ethyl]-N-[(4-methoxyphenyl)methyl]pyridin-2-amine
Traditional IUPAC Name
pyrilamine
SMILES
COC1=CC=C(CN(CCN(C)C)C2=NC=CC=C2)C=C1
Độ hòa tan
7.81e-01 g/l
logP
3.27
logS
-2.6
pKa (Strongest Basic)
8.76
PSA
28.6 Å2
Refractivity
87.74 m3·mol-1
Polarizability
32.89 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.85 (at 20 °C)
Cơ Chế Tác Dụng : Mepyramine (also known as pyrilamine) is a first generation antihistamine, targeting the H1 receptor. However, it rapidly permeates the brain and so often causes drowsiness as a side effect. It is used in over-the-counter combination products for colds and menstrual symptoms. Mepyramine is a histamine H1 receptor inverse agonist. It binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. Mepyramine competes with histamine for binding at H1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The sedative properties of Mepyramine occur at the subcortical level of the CNS.
Độc Tính : The signs and symptoms that are produced after the acute overdosage of Mepyramine include Convulsions, Coma, Ataxia, Hyperpyrexia, Tremor, Extrapyramidal effects, Excitement.
Chỉ Định : Mepyramine is a first generation antihistamine used in treating allergies, ymptomatic relief of hypersensitivity reaction, and in pruritic skin disorders.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06691
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08183
PharmGKB
http://www.pharmgkb.org/drug/PA165958366
Wikipedia
http://en.wikipedia.org/wiki/Mepyramine
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