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外観
白色, 結晶～結晶性粉末
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溶解性
水及びエタノールに溶け、ジエチルエーテルに溶けない。
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用途
コリン作動性アルカロイド剤
です。持続性ムスカリン様作用を有していま
す。また、腺分泌作用を示します。
-
用途
薬理研究用。
-
用途
コリン作動性アルカロイド剤 です。持続性ムスカリン様作用を有していま す。また、腺分泌作用を示します。
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効能
抗緑内障薬, 縮瞳薬, 唾液分泌促進薬, ムスカリン受容体作動薬
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商品名
サラジェン (キッセイ薬品工業); サラジェン (キッセイ薬品工業); サンピロ (参天製薬)
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化学的特性
Crystalline Solid
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使用
(+)-Pilocarpine hydrochloride is a muscarinic M1 and M2 acetylcholine receptor agonist with pKB values of 5 and 3.7, respectively. Systemic administration of (+)-Pilocarpine hydrochloride is typically used as an animal model for temporal lobe epilepsy and can mimic the generation of complex partial seizures by producing changes in hippocampal neuron morphology, membrane properties, and synaptic responses.
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一般的な説明
Pilocarpine monohydrochlorideis the hydrochloride of an alkaloid obtainedfrom the dried leaflets of Pilocarpus jaborandi or P. microphyllus,in which it occurs to the extent of about 0.5% togetherwith other alkaloids.
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生物活性
Muscarinic agonist.
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臨床応用
Pilocarpine, the salt of an alkaloid obtained from Pilocarpus jaborandi, is an example of a muscarinic agonist that does not adhere to the
traditional SAR. In 1876, Langley reported that extracts containing the alkaloid stimulated the end organs of parasympathetic neurons. The
structure of pilocarpine was reported in 1901.
Pilocarpine is marketed as tablets (Salogen), an ophthalmic solution, and gel. It penetrates the eye well and is the miotic of choice for
open-angle glaucoma and to terminate acute angle closure attacks. It also is used for the treatment of xerostomia (dryness of the mouth) caused
by radiation therapy of the head and neck, Sjogren's syndrome, or as a side effect of some psychotropic drugs.
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安全性プロファイル
Poison by ingestion,
intraperitoneal, and intravenous routes.
Experimental teratogenic and reproductive
effects. Human systemic effects: cardiac
changes. When heated to decomposition it
emits very toxic fumes of HCl and NOx.
See also PILOCARPINE.
