Coronaridine, also known as 18-carbomethoxyibogamine, is an

alkaloid Alkaloids are a class of basic, naturally occurring organic compounds that contain at least one nitrogen atom. This group also includes some related compounds with neutral and even weakly acidic properties. Some synthetic compounds of simila ...

found in ''

Tabernanthe iboga ''Tabernanthe iboga'' (iboga) is an evergreen rainforest shrub native to Central Africa. A member of the Apocynaceae family indigenous to Gabon, the Democratic Republic of Congo, and the Republic of Congo, it is cultivated across Central Africa ...

'' and related species, including ''

Tabernaemontana divaricata ''Tabernaemontana divaricata'', commonly called pinwheel flower, crape jasmine, East India rosebay, and Nero's crown, is an evergreen shrub or small tree native to South Asia, Southeast Asia and China. In zones where it is not hardy it is grown ...

'' for which (under the now obsolete synonym ''Ervatamia coronaria'') it was named. Like

ibogaine Ibogaine is a naturally occurring psychoactive substance found in plants in the family Apocynaceae such as '' Tabernanthe iboga'', '' Voacanga africana'', and '' Tabernaemontana undulata''. It is a psychedelic with dissociative properties. Pre ...

, (''R'')-coronaridine and (''S'')-coronaridine can decrease intake of cocaine and morphine intake in animals and it may have

muscle relaxant A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therap ...

and

hypotensive Hypotension is low blood pressure. Blood pressure is the force of blood pushing against the walls of the arteries as the heart pumps out blood. Blood pressure is indicated by two numbers, the systolic blood pressure (the top number) and the dias ...

activity.

Chemistry

Congeners

Coronaridine congers are important in drug discovery and development due to multiple actions on different targets. They have ability to inhibit Ca_v2.2 channel, modulate and inhibit subunits of nAChr selectively such as α9α10, α3β4 and potentiate GABA_A activity.

Pharmacology

Coronaridine has been reported to bind to an assortment of molecular sites, including: μ-opioid (K_i = 2.0 μM), δ-opioid (K_i = 8.1 μM), and

κ-opioid receptor The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP, is a G protein-coupled receptor that in humans is encoded by the ''OPRK1'' gene. The KOR is coupled to the G protein Gi/G0 and is one of four related receptors that bind ...

s (K_i = 4.3 μM),

NMDA receptor The ''N''-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel found in neurons. The NMDA receptor is one of three types of ionotropic glutamate receptors, the other two being AMPA and ...

(K_i = 6.24 μM) (as an

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, ri ...

), and

nAChR Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral ne ...

s (as an antagonist). It has also been found to inhibit the enzyme

acetylcholinesterase Acetylcholinesterase ( HGNC symbol ACHE; EC 3.1.1.7; systematic name acetylcholine acetylhydrolase), also known as AChE, AChase or acetylhydrolase, is the primary cholinesterase in the body. It is an enzyme that catalyzes the breakdown of ac ...

, act as a voltage-gated sodium channel blocker, and displays

estrogen Estrogen or oestrogen is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three major endogenous estrogens that have estrogenic hormonal ac ...

ic activity in rodents. In contrast to

and other

iboga alkaloid Iboga alkaloids are alkaloid constituents of ''Tabernanthe iboga''. Iboga alkaloids include ibogaine, tabernanthine, coronaridine, voacangine, ibogamine, and harmaline, among others. Noribogaine is a major active metabolite An active metabolite ...

s, coronaridine does not bind to either the σ₁ or σ₂ receptor.

Sources

References

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Pharmacodynamics Pharmacodynamics (PD) is the study of the biochemical and physiologic effects of drugs (especially pharmaceutical drugs). The effects can include those manifested within animals (including humans), microorganisms, or combinations of organisms ...

, list1 = {{Acetylcholine metabolism and transport modulators {{Estrogen receptor modulators {{Ion channel modulators {{Ionotropic glutamate receptor modulators {{Nicotinic acetylcholine receptor modulators {{Opioid receptor modulators Acetylcholinesterase inhibitors Alkaloids Alkaloids found in Iboga Carboxylate esters Ethers Nicotinic antagonists NMDA receptor antagonists Opioids Phytoestrogens Sodium channel blockers

Chemistry

Congeners

Pharmacology

Sources

See also

References