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Cyclopentolate HCl

Cat No.:V18957 Purity: ≥98%
Cyclopentolate (DL-Cyclopentolate) HCl is an atropine-like muscarinic receptor blocker (antagonist) with a pKb of 7.8 for ciliary muscle muscarinic receptors.
Cyclopentolate HCl
Cyclopentolate HCl Chemical Structure CAS No.: 5870-29-1
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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100mg
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Other Forms of Cyclopentolate HCl:

  • Cyclopentolate (DL-Cyclopentolate)
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Cyclopentolate (DL-Cyclopentolate) HCl is an atropine-like muscarinic receptor blocker (antagonist) with a pKb of 7.8 for ciliary muscle muscarinic receptors. Cyclopentolate HCl is an antimuscarinic agent widely used in ophthalmology.
Cyclopentolate hydrochloride is a synthetic anticholinergic agent commonly used in ophthalmology as a mydriatic and cycloplegic. It is an antagonist of muscarinic acetylcholine receptors. It is used to produce mydriasis and cycloplegia for ophthalmic diagnostic procedures. The compound has a molecular weight of 327.85 and a molecular formula of C17H25NO3·HCl.
Biological Activity I Assay Protocols (From Reference)
Targets
Cyclopentolate hydrochloride targets muscarinic acetylcholine receptors. It is an antagonist of muscarinic receptors with Ki values of 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively. By blocking these receptors, it causes mydriasis and cycloplegia.
ln Vitro
Cyclopentolate hydrochloride is an antagonist of muscarinic acetylcholine receptors with Ki values of 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively. By blocking these receptors, it causes mydriasis and cycloplegia.
ln Vivo
Rats pretreated with 20 mg/kg of cyclopentolate had a 90% survival rate [3].
Cyclopentolate hydrochloride is used in ophthalmology to produce mydriasis and cycloplegia for diagnostic procedures. It is commonly used as an eye drop during pediatric eye examinations to dilate the eye and prevent the eye from focusing/accommodating.
Enzyme Assay
Cyclopentolate hydrochloride is evaluated in cell-free receptor binding assays to determine its affinity for muscarinic receptors. Radioligand binding displacement assays are performed using membrane preparations expressing muscarinic receptor subtypes. Ki values are determined to quantify the potency of receptor antagonism.
Cell Assay
Cyclopentolate hydrochloride is assessed in cell-based assays to measure its antagonist activity at muscarinic receptors. Cells expressing muscarinic receptors are treated with Cyclopentolate hydrochloride, and receptor activity is measured by assessing downstream signaling pathways.
Animal Protocol
Animal/Disease Models: 80 SD (SD (Sprague-Dawley)) rats (acute lethal organophosphorus pesticide (OP) poisoning model) [3]
Doses: 20 mg/kg (cyclopentolate for ophthalmic use)
Route of Administration: intraperitoneal (ip) injection
Experimental Results: with The survival rate of rats pretreated with ocular cyclopentolate (20 mg/kg) was 90%.
Cyclopentolate hydrochloride is administered as eye drops in animal models and in clinical settings to evaluate its mydriatic and cycloplegic effects. It is used in ophthalmic diagnostic procedures.
ADME/Pharmacokinetics
Cyclopentolate hydrochloride has a molecular weight of 327.85 and a molecular formula of C17H25NO3·HCl. It has a CAS number of 5870-29-1. The compound is a synthetic anticholinergic agent.
Toxicity/Toxicokinetics
No detailed toxicity data is available for Cyclopentolate hydrochloride beyond its known use as an ophthalmic agent. The compound is a therapeutic agent and is not for research purposes only. It is generally well-tolerated for ophthalmic use.
References

[1]. Öner V, Bulut A, Öter K. The effect of topical anti-muscarinic agents on subfoveal choroidal thickness in healthy adults. Eye (Lond). 2016;30(7):925‐928.

[2]. Ishikawa H, DeSantis L, Patil PN. Selectivity of muscarinic agonists including (+/-)-aceclidine and antimuscarinics on the human intraocular muscles. J Ocul Pharmacol Ther. 1998;14(4):363‐373.

[3]. Öner V, Bulut A, Öter K. The effect of topical anti-muscarinic agents on subfoveal choroidal thickness in healthy adults. Eye (Lond). 2016;30(7):925‐928.

Additional Infomation
Cyclopentolate hydrochloride is the hydrochloride salt of Cyclopentolate. It is used in ophthalmic diagnostic procedures to achieve therapeutic effects through mydriasis (excessive pupillary dilation) and cycloplegia (cycloplegic retraction). It has a faster onset of action and a shorter duration of action than atropine. It has multiple uses, including mydriatic, parasympathetic blocker, diagnostic agent, and muscarinic receptor antagonist. It contains the Cyclopentolate group. Cyclopentolate hydrochloride is the hydrochloride form of Cyclopentolate (an anticholinergic drug). After instillation, Cyclopentolate hydrochloride blocks acetylcholine receptors in the iris sphincter and ciliary muscle, preventing their contraction. This causes pupillary dilation, producing mydriasis, and prevents eye accommodation. A parasympathetic blocker, an anticholinergic drug used only to induce mydriasis or cycloplegia. See also: Cyclopentolate (containing the active ingredient)... See more...
Cyclopentolate hydrochloride is a synthetic anticholinergic agent used in ophthalmology as a mydriatic and cycloplegic. It has a CAS number of 5870-29-1. It is an antagonist of muscarinic acetylcholine receptors. It is a therapeutic agent.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H25NO3.HCL
Molecular Weight
327.84624
Exact Mass
327.16
CAS #
5870-29-1
Related CAS #
Cyclopentolate;512-15-2
PubChem CID
22162
Appearance
White to off-white solid powder
Boiling Point
409.7ºC at 760mmHg
Melting Point
137-141°
Flash Point
201.5ºC
LogP
2.982
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
7
Heavy Atom Count
22
Complexity
331
Defined Atom Stereocenter Count
0
InChi Key
RHKZVMUBMXGOLL-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H25NO3.ClH/c1-18(2)12-13-21-16(19)15(14-8-4-3-5-9-14)17(20)10-6-7-11-17;/h3-5,8-9,15,20H,6-7,10-13H2,1-2H3;1H
Chemical Name
2-(dimethylamino)ethyl 2-(1-hydroxycyclopentyl)-2-phenylacetate;hydrochloride
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~250 mg/mL (~762.54 mM)
H2O : ~100 mg/mL (~305.02 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 100 mg/mL (305.02 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0502 mL 15.2509 mL 30.5018 mL
5 mM 0.6100 mL 3.0502 mL 6.1004 mL
10 mM 0.3050 mL 1.5251 mL 3.0502 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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