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Pargyline

Pargyline structure

CAS No:
555-57-7
Formula:
C11H13N
Chemical Name:
Pargyline
Synonyms:
Benzenemethanamine,N-methyl-N-2-propyn-1-yl-;Benzylamine,N-methyl-N-2-propynyl-;Benzenemethanamine,N-methyl-N-2-propynyl-;N-Methyl-N-2-propyn-1-ylbenzenemethanamine;N-Benzyl-N-methyl-2-propynylamine;N-Methyl-N-benzylpropynylamine;N-Methyl-N-2-propynylbenzylamine;Pargylamine;Pargylin;Pargyline;N-Methyl-N-propargylbenzylamine;Supirdyl;Eudatin;Benzylmethylpropargylamine;N-Benzyl-N-methylpropargylamine;N-Methyl-N-2-propynylbenzenemethanamine
Categories:
Organic Chemistry > Amides

Description

Pargyline is an irreversible non-selective monoamine oxidase (MAO) inhibitor drug (IC50 for MAO-A is 11.52 nM and for MAO-B is 8.2 nM) .

Solid

Pargyline is an aromatic amine.|Pargyline is a monoamine oxidase inhibitor with antihypertensive properties.|Pargyline is a monoamine oxidase (MAO) inhibitor with antidepressant activity. Pargyline selectively inhibits MAO type B, an enzyme catalyzing the oxidative deamination and inactivation of certain catecholamines, such as norepinephrine and dopamine, within the presynaptic nerve terminals. By inhibiting the metabolism of these biogenic amines in the brain, pargyline increases their concentration and binding to postsynaptic receptors. Increased receptor stimulation may cause downregulation of central receptors which may attribute to pargyline's antidepressant effect.|A monoamine oxidase inhibitor with antihypertensive properties.

Pargyline Basic Attributes

Molecular Weight：

159.23

Exact Mass：

159.23

EC Number：

209-101-6

UNII：

9MV14S8G3E

DSSTox ID：

DTXSID3023423

NCI Thesaurus Code：

C66322

ATC Code：

C - Cardiovascular system

HScode：

29214900

Characteristics

PSA：

3.2

XLogP3：

1.75160

Appearance：

Clear yellow Liquid

Density：

1.0291 g/cm³ @ Temp: 20 °C

Melting Point：

15-20 °C

Boiling Point：

96.5 °C

Flash Point：

183 °F

Refractive Index：

n20/D 1.522(lit.)

Water Solubility：

9.98e-02 g/L

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

UN 2810 6.1/PG 3

wgk germany：

hazard class code：

23/24/25-36/37/38-22

safety instructions：

26-36/37/39-45-23

RTECS Number：

DP6475000

Marks：

Precautionary statement(s)：

P261, P264, P270, P271, P280, P301+P310, P302+P352, P304+P340, P305+P351+P338, P311, P312, P321, P322, P330, P332+P313, P337+P313, P361, P362, P363, P403+P233, P405, P501

Hazard Statements：

H301

GHS Classification：

|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P310, P302+P352, P304+P340, P305+P351+P338, P311, P312, P321, P322, P330, P332+P313, P337+P313, P361, P362, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 40 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

For the treatment of moderate to severe hypertension.

Drug Transformations：

Pargyline has known transformation products that include Pargyline-N-oxide.

Pharmacology：

Pargyline is a monoamine oxidase B (MAO-B) inhibitor with antihypertensive properties. Patients taking pargyline must avoid concurrent consumption of tyramine-containing foods such as bleu cheese and beer, as this can lead to a hypertensive crisis.

MeSH：

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)|A chemically heterogeneous group of drugs that have in common the ability to block oxidative deamination of naturally occurring monoamines. (From Gilman, et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p414) (See all compounds classified as Monoamine Oxidase Inhibitors.)

Mechanism of Action：

MAOIs act by inhibiting the activity of monoamine oxidase, thus preventing the breakdown of monoamine neurotransmitters and thereby increasing their availability. There are two isoforms of monoamine oxidase, MAO-A and MAO-B. MAO-A preferentially deaminates serotonin, melatonin, epinephrine and norepinephrine. MAO-B preferentially deaminates phenylethylamine and trace amines. Pargyline functions by inhibiting the metabolism of catecholamines and tyramine within presynaptic nerve terminals. Catecholamines cause general physiological changes that prepare the body for physical activity (fight-or-flight response). Some typical effects are increases in heart rate, blood pressure, blood glucose levels, and a general reaction of the sympathetic nervous system.

MeSH Entry Terms：

Hydrochloride, Pargyline

Pargyline Use and Manufacturing

Uses

analgesic

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals -> Nervous System -> Analgesics

Computed Properties

Molecular Weight:159.23
XLogP3:2.1
Hydrogen Bond Acceptor Count:1
Rotatable Bond Count:3
Exact Mass:159.104799419
Monoisotopic Mass:159.104799419
Topological Polar Surface Area:3.2
Heavy Atom Count:12
Complexity:159
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Material

Benzaldehyde

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