Tropicamide

English synonyms

Tropicamide(200mg);(2R)-N-ethyl-3-hydroxy-2-phenyl-N-(pyridin-4-ylMethyl)propanaMide;
TROPICAMIDUM;TropicaMideN-Ethyl-3-hydroxy-2-phenyl-N-(pyridin-4-ylMethyl)propanaMide;TropicamideforpeakidChemicalbookentification;
n-ethyl-2-phenyl-n-(4-pyridylmethyl)-hydracrylamid;
N-Ethyl-3-hydroxy-2-phenyl-N-(4-pyridinylmethyl)propanamide;
n-ethyl-alpha-(hydroxymethyl)-n-(4-pyridinylmethyl)-benzeneacetamid

CAS number

1508-75-4

Molecular formula

C17H20N2O2

Molecular weight

284.35

EINECS number

216-140-2

Melting point

98℃

Boiling point

492.8±45.0°℃(Predicted)

Density

1.161±0.06 g/cm3(Predicted)

Storage conditions

2-8℃

Solubility

Solubility of 2-hydroxypropyl-β-cyclodextrin in 45% (w/v) aq: 4.3 mg/mL

Acidity coefficient (pKa)

pKa 5.3 (Uncertain)

Form

Solid

Color

White

Water solubility

0.2g/L(25℃)

Maximum wavelength (λmax)

254nm(HCl aq.)(lit.)

Merck

149780

InChl

InChl=1S/C17H20N202/c1-2-19(12-14-8-10-18-11-9-14)17(21)16(13-20)
15-6-4-3-5-7-15/h3-11,16,20H,2, 12-13H2,1H3

InChlKey

BGDKAVGWHJFAGW-UHFFFAOYSA-N

SMILES

C(CO)(C(=O)N(CC)CC1=CC=NC=C1)C1C=CC=CC=1

Ophthalmic drugs

Tropicamid is an anticholinergic drug. It is a white crystalline powder at room temperature. It is odorless, slightly soluble in water,
and easily soluble in ethanol, dilute hydrochloric acid, dilute sulfuric acid and chloroform. It can block the excitation of the iris sphincter and ciliary muscle
caused by acetylcholine. Its 0.5% solution can cause mydriasis; 1% solution can cause ciliary muscle paralysis and mydriasis. It is mainly used clinically to treat mydriasis and
accommodation paralysis. Tropicamide is a synthetic derivative of tropic acid. It has a low dissociation constant, good intraocular permeability, and strong tissue diffusion,
which may be the reason for its rapid onset and short duration. The mydriasis and accommodation paralysis effects of 0.5% and 1% solutions of this product reach a peak
within 20-30 minutes after eye drops. The effect gradually decreases afterwards, and the accommodation paralysis (residual) lasts for 2 to 6 hours. Mydriasis (residual) lasts
for about 7 hours. Tropicamide is a drug similar to atropine, so it can cause a sharp increase in intraocular pressure in angle-closure glaucoma, and may also stimulate undiagnosed
angle-closure glaucoma. The intensity of the ciliary muscle accommodation paralysis effect of tropicamide eye drops is closely related to the dose, and its four concentrations of 0.25%,
0.5%, 0.75% and 1% all have accommodation paralysis effects. After eye drops, the maximum residual accommodation degrees are 3.17 diopters for 0.25% and 1.30 diopters for 1%.
For those who can maintain the residual accommodation degree at or below 2.0 diopters, 0.75% and 1% solutions can maintain it for 40 minutes, and 0.5% for about 15 minutes.
fter a drop of 1% solution is dropped into the eye, it is dropped again after 5 to 25 minutes, which can obtain a more satisfactory ciliary muscle paralysis
ffect for about 20 to 30 minutes.After 2 to 6 hours, you can read books and newspapers, and the accommodation function will return to the level before the drop within 6 hours.

Biological Activity

Tropicamide is an anticholinergic, selective antagonist of the muscarinic receptor M4 subtype with an IC50 of 8.0 nM.

Target

Target

Value

Value

8 nM

Uses

Used as anticholinergic, mydriatic

Uses

M4 muscarinic acetylcholine receptor antagonist.

Dangerous goods symbol

Xn,Xi

Hazard category code

20/21/22-36/37/38-42/43-41-37/38-22

Safety instructions

22-26-36-36/37/39

WGK Germany

3

RTECS number

CY1487860

Customs code

29333990

Upstream Raw Materials

Ethylamine, Hydrochloric Acid, Aminopyridine Impurity 223, Acetyl Tropicamide, Ethyl 2-phenyl-malonate, N-(4-pyridylmethyl)ethylamine, Tropicic Acid, Diethyl Phenylmalonate, 4-pyridinecarboxaldehyde