(+)-Пилокарпин гидрохлорид

Химические свойства

Crystalline Solid

Использование

(+)-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.

Общее описание

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.

Биологическая активность

Muscarinic agonist.

Клиническое использование

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.

Профиль безопасности

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.