Ph Ch 128

Front 1

trial and error

Back 1

Until the mid-20th century, the discovery of bioactive entities from plants was largely the result of a ___ process, without much understanding of their mechanism of action in vertebrate physiological systems.

Front 2

Opium
analgesic
morphine

Back 2

___, the dried latex of the capsules of Papaver somniferum L. has been used for its __properties for several millennia, with the major active narcotic analgesic alkaloid __being isolated at the beginning of 19th century.

Front 3

opioid

opiates

Back 3

It was only in 1973 that the ___ receptors were characterized, thus helping to explain the mode of action of ___

Front 4

secondary metabolites
“biochemical tools” or “pharmacological probes.”

Back 4

In a similar fashion, plant ___have helped define many receptor types and have served as invaluable tools to help elucidate biological processes. These types of compounds are known as ____

Front 5

pilocarpine;physostigmine; (−)-hyoscyamine; nicotine;

muscarine
receptor-ligand

Back 5

The isolation of pure plant natural products, such as, ___, ___,___, and ___, and the fungal isolate, ___, played a major role in the devtof modern pharmacology by enabling the discovery of intricate ___ mechanisms

Front 6

psychoactive

Back 6

Natural products, including some traditionally known to have ___ properties, have provided many potent CNS-active agents

Front 7

in silico
receptorome psychoactive

Back 7

Based on the contribution of plant __cpds in the understanding of neurochemical processes, ___ methods for screening the ___ for plant-derived cpds have been suggested to further elucidate and define molecular mechanisms.

Front 8

marijuana
Cannabis sativa L.

Back 8

The cannabinoid-type psychoactive principles of __ , (scientific name____) have been of interest to pharmacologists for many years

Front 9

(−)-Δ9-trans-tetrahydrocannabinol
cannabinoid

Back 9

The biological characterization of the major euphoriant principle, ___ (THC), has led to an understanding of the molecular mechanisms of these compounds, and ultimately enabled the characterization of the __receptor (CB1)

Front 10

rimonabant
obesity

Back 10

The first selective antagonist inverse agonist at the CB1 receptor, ___, was recently approved in
the European Union for the treatment of ___ and metabolic disorder.

Front 11

Cocaine
dopamine transport protein
anesthetic
sodium

Back 11

___, from Erythroxylum coca Lam., besides causing euphoria by inhibiting the __ responsible for its recreational and illegal use, exerts a local __activity through blocking __ channels and is still used as a probe for this target.

Front 12

Erythroxylum coca Lam

Back 12

Cocaine is isolated from ___

Front 13

salvinorin A
Salvia divinorum Epling and Jativa

Back 13

The discovery of a potent and selective κ-opioid receptor agonist compound, ___, a hallucinogenic neoclerodane diterpenoid from___ and__, is the first nonnitrogenous compound found to demonstrate this type of activity

Front 14

cathinone
Catha edulis Forssk. (khat)
biogenic amine

Back 14

Chiral protoalkaloids, such as __, a psychotropic constituent of __, have provided probes 4 studying d mechanistic properties of __ transp & afforded info regarding the effect of stereochem at transportation level of nitrogenous cpds

Front 15

d -Tubocurarine
Chondodendron tomentosum Ruiz and Pav. (curare)
nicotinic acetylcholine
5-hydroxytryptamine

Back 15

__, isolated from a South American plant used as arrow poison,__, is no longer employed as a skel. musc. relaxant drug, is still used in pharmacolog studies as a competitive agonist of ___ receptors and also as an agonist of the ___ receptor

Front 16

Muscimol
Amanita muscaria
gaboxadol

Back 16

___, a centrally acting principle of the mushroom ___ (fly agaric), is known to be a potent GABAA receptor agonist and led to the development of a bicyclic analogue, ___, a drug currently in phase III clinical trials for the treatment of sleep disorders.

Front 17

Bicuculline
picrotoxinin

Back 17

___(Dicentra cucullaria Bernh.) and ___, on the other hand, serve as potent antagonists at GABAA receptors.

Front 18

Strychnine
Strychnos nux-vomica L

Back 18

____, the toxic principle of ___., has proven to be useful in the studies on glycine (Gly) receptors as a competitive antagonist of this receptor type at nM levels

Front 19

chalcone
p53/MDM2
ligase

Back 19

Members of the ___subtype of flavonoids have provided useful tools for probing the___system through the inhibition of ubiquitin___.

Front 20

Quisqualic acid

Back 20

___ (Quisqualis indica L.) is a potent agonist for
the ionotopic glutamate (iGlu) receptors

Front 21

Epigenetic modulation

Back 21

___ is important for the treatment of cancer and the
understanding of cancer cell dynamics

Front 22

DNA-methyl transferase (DNMT)

Back 22

DNA-methylation is regulated by the___ family of enzymes which constitute potential targets with antiproliferative outcome in cancer chemotherapy.

Front 23

(−)-Epigallocatechin-3-gallate (EGCG)
(Camellia sinensis Kuntze)

Back 23

___ from ____, and other flavan derivatives have been shown to be DNMT1 inhibitors at μM levels

Front 24

Curcumin
(Curcuma longa L.)
histone acetyl transferase (HAT)

Back 24

___ from ___ has been found to act as a ____ inhibitor, leading to transcriptional silencing

Front 25

Genistein
Leguminosae
protein tyrosine kinases
angiogenesis

Back 25

___, an isoflavone found in plants of the family ___, is an inhibitor of several ___ and is currently in phase II clinical trials for its potential as an __
inhibitor

Front 26

Genistein
cyclicnucleotide

Back 26

___also has been utilized as a probe to identify binding sites for PTKs by observing the effect it demonstrates on ___- gated channels

Front 27

phorbol
Croton tiglium L.
12-O-tetradecanoylphorbol-13-acetate
protein kinase C
carcinogenesis

Back 27

Long-chain ester derivatives of ___, a tetracyclic diterpene from the seed oil of___, and its most abundant rep. , ___, are potent activators of ____ (PKC) & are used as std. tumor promoters for study of experimental ___ in animal models.

Front 28

capsaicin
(Capsicum spp.)
resiniferatoxin from Euphorbia resinifera Berg.
transient receptor potential
vanilloid

Back 28

Investigations on capsaicin (66), the vanillyl-group containing “hot” principle in chili peppers __, as well as the irritant compound __ from ___ have led to the characterization of___channels and the ___receptors (TRPV1).

Front 29

chronic pain

Back 29

TRP and TRPV1 receptors show the possibility of serving as new targets to assist with diseases that involve ___

Front 30

(−)-menthol (68) (Mentha spicata L.)
cold
TRPM8

Back 30

While ligands acting on TRPV1 cause a burning sensation, compounds with a cooling effect, such as ___ have led to the characterization of ___sensors, most importantly the ___ receptor, which also plays a role in the nociceptive process