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Pharmacologic characteristic
Functional selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity
Functional_selectivity
Chemical which binds to and activates a biochemical receptor
type. Terms that describe this phenomenon are "functional selectivity", "protean agonism", or selective receptor modulators. As mentioned above, agonists
Agonist
Subtype of serotonin receptor
animal studies. TCB-2 25C-NBOMe 25CN-NBOH – 100× selectivity for 5-HT2A over 5-HT2C, 46× selectivity over 5-HT2B. 3-Carboxy indole PB-22 (1-pentyl-indole-3-carboxylic
5-HT2A_receptor
Topics referred to by the same term
selectivity, in pharmacology Functional selectivity, in pharmacology Natural selection, in biology Reactivity–selectivity principle, in general chemistry
Selectivity
Class of psychoactive drugs
4-benzodiazepine. The functional selectivity is not unique to the nonbenzodiazepine structural class and has more to do with selectivity among different types
Nonbenzodiazepine
Psychoactive chemical
This differential strategy has been given several names, including functional selectivity and biased agonism. The first opioid that was intentionally designed
Opioid
Atypical antipsychotic medication
consistent with the hypothesis that aripiprazole has "functionally selective" actions. The "functional-selectivity" hypothesis proposes that a mixture of agonist/partial
Aripiprazole
Class of drugs
differences between AAS in terms of their intracellular metabolism, functional selectivity (differential recruitment of coactivators), and non-genomic mechanisms
Anabolic_steroid
Agent in biochemistry
(2018-08-06). "Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity". International Journal of Neuropsychopharmacology. 21 (10): 962–977
Inverse_agonist
Type of receptor ligand or drug that blocks a biological response
models with intermediate conformational states. The discovery of functional selectivity and that ligand-specific receptor conformations occur and can affect
Receptor_antagonist
In biochemistry, the preference of ligands to bind with one receptor over another
chemistry, binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how a ligand
Binding_selectivity
Drug class
However, highly selective serotonin 5-HT2A receptor agonists, such as TGF-8027, have also been developed. In addition to degree of selectivity for the serotonin
Serotonin 5-HT2A receptor agonist
Serotonin_5-HT2A_receptor_agonist
Protein-coding gene in humans
the first demonstration of functional selectivity with dopamine receptors. Dinapsoline – full agonist with 5-fold selectivity for D1-like receptors over
Dopamine_receptor_D1
Pharmaceutical compound
weak partial agonist. It shows varying activational efficacies or functional selectivity at GABAA receptors of different α subunit compositions, with EmaxTooltip
Imidazoleacetic_acid
tools to synthesize functionalized aromatic compounds with high selectivity. The widely used approach to achieve ortho-selectivity involves metal-chelating
Meta-selective C–H functionalization
Meta-selective_C–H_functionalization
Species of plant
the μ-opioid receptor than mitragynine. These compounds display functional selectivity and do not activate the β-arrestin pathway which may be partly responsible
Mitragyna_speciosa
Proteins activated by the hormone estrogen
subtypes can transactivate transcription only when a heterodimer with the functional ERß1 receptor of 59 kDa is formed. The ERß3 receptor was detected at high
Estrogen_receptor
Drug class
concentration that is required to stimulate the 2C receptors. This functional selectivity is critical to prevent potential side effects and suggests that
5-HT2C_receptor_agonist
Chemical compound
that this might be due to its low intrinsic efficacy, rather than functional selectivity or 'G protein bias' as initially reported. In tests on mice, PZM21
PZM21
Topics referred to by the same term
Functional agonist may refer to: functional selectivity Physiological agonism This disambiguation page lists articles associated with the title Functional
Functional_agonist
Mammalian protein found in Homo sapiens
~10-fold selectivity over 5-HT2A and 5-HT2C BW-723C86 – 100-fold selectivity over 5-HT2A but only 3- to 10-fold selectivity over 5-HT2C, fair functional subtype
5-HT2B_receptor
Chemical compound
known as NLX-101, is a potent and selective 5-HT1A receptor full agonist. In addition, it displays functional selectivity, or biased agonism, by preferentially
F-15599
Class of medications
relies on xanomeline's functional selectivity for the M1 and M4 muscarinic receptors, with trospium chloride, a peripherally selective antimuscarinic added
Antipsychotic
Chemical compound
receptor. It binds to α1, α2, α3 and α5 -containing subtypes, with functional selectivity for α5-containing subtypes. Administration of α5IA following alcohol
Α5IA
in high selectivity based on innate substrate selectivity for a given reaction or based on catalyst control. The discovery of site-selective LSF reactions
Late-stage_functionalization
Chemical compound
It is a non-selective agonist of all five muscarinic acetylcholine receptors with similar affinities. However, functional selectivity for the M1 receptor
Sabcomeline
Chemical compound
It is a selective agonist for the androgen receptor, producing functional selectivity with effective dissociation of anabolic and androgenic effects,
LGD-3303
Computational quantum mechanical modelling method to investigate electronic structure
Density functional theory (DFT) is a computational quantum mechanical modeling method used in physics, chemistry and materials science to investigate the
Density_functional_theory
Class of opioid receptors found in humans
has enabled structure-based design of a new class of opioids with functional selectivity. Three variants of the μ-opioid receptor are well characterized
Mu-opioid_receptor
Central nervous system stimulant
Hasenhuetl PS, Bhat S, Freissmuth M, Sandtner W (March 2019). "Functional Selectivity and Partial Efficacy at the Monoamine Transporters: A Unified Model
Amphetamine
Pharmaceutical compound
given intravenously. The drug acts as a selective biased partial agonist of the MOR, with functional selectivity for activation of G protein signaling over
Susineridine
Main receptor for most antipsychotic drugs
Cariprazine Cannabidiol GSK-789,472 – Also D3 antagonist, with good selectivity over other receptors Ketamine (also NMDA antagonist) LSD – in vitro,
Dopamine_receptor_D2
Branch of pharmacology
pathological conditions - long term structural or functional changes Disturbed homeostasis Functional selectivity (biased Agonism) - preferentially activate
Pharmacodynamics
Psychedelic drug
block the psychedelic effects of LSD. The drug exhibits pronounced functional selectivity or biased agonism at the serotonin 5-HT2A and 5-HT2C receptors in
LSD
Psychedelic drug
M, Nichols DE, Kobilka B, Weinstein H, et al. (January 2007). "Functional selectivity and classical concepts of quantitative pharmacology". The Journal
Dimethyltryptamine
Chemical compound
initially classified as a selective H3 antagonist, but newer research (2005) suggests also agonist properties, i.e., functional selectivity. The relatively recent
Cipralisant
Topical nasal decongestant
"Exploring the determinants of trace amine-associated receptor 1's functional selectivity for the stereoisomers of amphetamine and methamphetamine". J Med
Levomethamphetamine
Chemical compound
pathway but does not recruit the β-arrestin pathway. Due to its functional selectivity for the G protein pathway, 6′-GNTI functions as an antagonist of
6'-Guanidinonaltrindole
Antidepressant medication
PN, Kroeze WK, Farrell MS, Roth BL (October 2011). "Antagonist functional selectivity: 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A
Mirtazapine
Sauls, HR; Triantafillou, JA (1994). "a non-steroidal estrogen with functional selectivity for bone over uterus in rats". J Med Chem. 37 (11): 1550–2. doi:10
Timeline of cancer treatment development
Timeline_of_cancer_treatment_development
Chemical compound
κ-opioid receptor (KOR), resulting in very high potency. It is functionally selective, activating G proteins more potently than β-arrestin-2. RB-64 has
RB-64
Chemical compound
led to the obtainment of new derivatives endowed with binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype. Wheeler,
Anabaseine
Mammalian protein found in Homo sapiens
assessed as H3 antagonist, later found to be an agonist, shows functional selectivity, activating some G-protein coupled pathways but not others) GT-2203
Histamine_H3_receptor
Class of chemical compounds
5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors". J Med Chem. 57 (12): 5258–5269
Substituted_3-benzazepine
Sleep medication
4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent
Zolpidem
Group of chemical compounds
agonists. 22-Thiocyanato-salvinorin A is notable because of its functional selectivity. Salvinorin B methoxymethyl ether is seven times more potent than
Salvinorin
Head movement in rodents upon 5-HT2A receptor activation
behavioral differences between LSD and lisuride may be due to 5-HT2A functional selectivity, whereby lisuride activates the 5-HT2A receptor but does not recruit
Head-twitch_response
Theory of motivation
Socioemotional selectivity theory (SST; developed by Stanford psychologist Laura L. Carstensen) is a life-span theory of motivation. The theory maintains
Socioemotional selectivity theory
Socioemotional_selectivity_theory
Chemical compound
respectively. As such, its binding selectivity for the ERβ over the ERα was 7-fold and its functional selectivity for the ERβ over the ERα was between
DCW234
Chemical compound
selectivity and 11-fold functional selectivity for the ERβ over the ERα. An enantiomer of SERBA-2, erteberel (SERBA-1), is more potent and selective in
SERBA-2
Mammalian protein found in Homo sapiens
(NADA). Many of these ligands appear to exhibit properties of functional selectivity at the CB2 receptor: 2-AG activates the MAPK-ERK pathway, while
Cannabinoid_receptor_2
Typical antipsychotic drug of the thioxanthene class
lower doses are not well understood; however, it may be mediated by functional selectivity and/or preferentially binding to D2 autoreceptors at low doses,
Flupentixol
Chemical compound
not inhibit the enzyme GABA transaminase (GABA-T). The drug shows functional selectivity at the GABAA receptor relative to GABA itself, activating GABAA
Gaboxadol
Chemical compound
A.; Lee, Yong Sok; Kunos, George; Cinar, Resat (11 June 2021). "Functional Selectivity of a Biased Cannabinoid-1 Receptor (CB 1 R) Antagonist". ACS Pharmacology
Monlunabant
Disorder of decreased tolerance to specific sounds
Misophonia (or selective sound sensitivity syndrome) is a disorder of decreased tolerance to specific sounds or their associated stimuli, or cues. These
Misophonia
Impairment in the ability to learn new faces
neuropsychology of face perception: beyond simple dissociations and functional selectivity. Philosophical Transactions of the Royal Society B-Biological Sciences
Prosopamnesia
fields and Functional Architecture of Monkey Striate Cortex’, The Journal of Physiology 195(1), 215-243 T. Lindeberg (2025) "Orientation selectivity properties
Orientation_selectivity
Opioid analgesic drug
that this might be due to its low intrinsic efficacy, rather than functional selectivity or 'G protein bias', although the validity of that conclusion has
Oliceridine
Australian pharmacologist and toxicologist
(with Appendix by S. Watson) (2012) A simple method to quantify functional selectivity and agonist bias. ACS Chem. Neurosci. 3: 193-203 Wootten D., Savage
Arthur_Christopoulos
US military chemical warfare research
Keith J.; Spedding, Michael; Mailman, Richard B. (January 2007). "Functional Selectivity and Classical Concepts of Quantitative Pharmacology". Journal of
Edgewood Arsenal human experiments
Edgewood_Arsenal_human_experiments
Naturally occurring psychedelic compound
Sáez-Briones P, Reyes-Parada M, Cassels BK, et al. (June 2007). "Functional selectivity of hallucinogenic phenethylamine and phenylisopropylamine derivatives
Mescaline
Psychedelic drug
Sáez-Briones P, Reyes-Parada M, Cassels BK, et al. (June 2007). "Functional selectivity of hallucinogenic phenethylamine and phenylisopropylamine derivatives
2C-B
American pharmaceutical company
patent number US10562853B2. The NCEs are selective serotonin 5-HT1A receptor agonists that show functional selectivity for either extracellular signal-regulated
Neurolixis
Atypical antipsychotic medicine
(2017). "Aripiprazole, A Drug that Displays Partial Agonism and Functional Selectivity". Current Neuropharmacology. 15 (8): 1192–1207. doi:10
Cariprazine
5-HT2C receptor agonist
significant activity at other serotonin receptors. BMB-101 shows functional selectivity at the serotonin 5-HT2C receptor for activation of Gq signaling
BMB-101
Pharmaceutical compound
treatment of neuropathic pain. However, it is also believed to show functional selectivity as it showed reduced levels of sedation and of other animal surrogates
Z8526711350
Class of cell surface receptors coupled to G-protein-associated intracellular signaling
depends on the ligand that is bound to the GPCR, this is called functional selectivity (also known as agonist-directed trafficking, or conformation-specific
G_protein-coupled_receptor
of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype". European
Alpha-3 beta-4 nicotinic receptor
Alpha-3_beta-4_nicotinic_receptor
Chemical compound
DAR-0100) is a moderately selective full agonist at the dopamine D1 and D5 receptors. It has approximately 10-fold selectivity for D1 and D5 over the D2
Dihydrexidine
Drug class
receptor 2 (SSTR2). This is a display of functional selectivity at the SSTR2 receptor. Functional selectivity is the effect of one ligand having one agonism
Broad-spectrum chemokine inhibitor
Broad-spectrum_chemokine_inhibitor
Chemical compound
14-fold binding selectivity for the ERβ over the ERα (Ki = 0.19 nM versus 2.68 nM, respectively). However, it shows 32-fold functional selectivity for activation
Erteberel
American biopharmaceutical company
approach to drug discovery is based on utilizing ligand bias, or functional selectivity, at GPCR targets to produce drugs with improved efficacy and reduced
Trevena,_Inc.
American pharmacologist
powerful anti-inflammatory effects and that this effect is mediated by functionally selective activation of serotonin 5-HT2A receptors. Moreover, he found that
Charles_D._Nichols
Chemical compound in the ergot family of alkaloids
posited to be due to functional selectivity at the serotonin 5-HT2A receptor. However, ergotamine is also peripherally selective, which may instead account
Ergotamine
MRI procedure that measures brain activity by detecting associated changes in blood flow
Functional magnetic resonance imaging or functional MRI (fMRI) measures brain activity by detecting changes associated with blood flow. This technique
Functional magnetic resonance imaging
Functional_magnetic_resonance_imaging
Pharmaceutical compound
acid (GABA). The drug is a potent and selective GABAA receptor partial agonist. It shows functional selectivity at GABAA receptors of different α subunit
Piperidine-4-sulfonic_acid
Type of nonsteroidal anti-inflammatory drug
(COX-2), an enzyme responsible for inflammation and pain. Targeting selectivity for COX-2 reduces the risk of peptic ulceration and is the main feature
Cyclooxygenase-2_inhibitor
Chemical compound
which is an orally active, potent, and selective agonist for androgen receptors (Ki 2.1nM, 20x functional selectivity for muscle tissue over prostate) and
BMS-564,929
Pharmaceutical compound
preferences to provide an insight into the structural basis of functional selectivity. The outcomes showed that the type of ligand interaction with the
5-Phenoxytryptamine
Pharmaceutical compound
(June 2016). "A single-chain derivative of the relaxin hormone is a functionally selective agonist of the G protein-coupled receptor, RXFP1". Chemical Science
B7-33
Investigational substance-related disorder drugs
KB-128 - AdisInsight KB-128 - Synapse Jeremy Forest. "Novel and functionally selective 5-HT2C receptor agonist for treating Alcohol Use Disorder". RePORTER
List of investigational substance-related disorder drugs
List_of_investigational_substance-related_disorder_drugs
Chemical compound
It has similar binding affinity to 5-HT2A and 5-HT2C but shows functional selectivity for 5-HT2C. Lorcaserin PHA-57378 SCHEMBL5334361 WAY-163909 WAY-261240
WAY-470
Drug; KOR biased agonist
"Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential". Journal of Medicinal
KSC-12-192
Serotonin receptor protein distributed mainly in the choroid plexus
5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors". Journal of Medicinal Chemistry
5-HT2C_receptor
perspective, each of these pollinators are functionally equivalent and thus are not subjected to specific selective pressures Variation in the shape and structure
Functional equivalence (ecology)
Functional_equivalence_(ecology)
CNS stimulant and isomer of amphetamine
"Exploring the determinants of trace amine-associated receptor 1's functional selectivity for the stereoisomers of amphetamine and methamphetamine". J Med
Levoamphetamine
Ion channel that selectively passes K+
remove the hydration shell from the ion when it enters the selectivity filter. The selectivity filter is formed by a five residue sequence, TVGYG, termed
Potassium_channel
Chemical compound
testosterone or anabolic steroids. S-40503 is a SARM that shows good functional selectivity for bone tissue, and has relatively little effect on muscle mass
S-40503
KB-128 - AdisInsight KB-128 - Synapse Jeremy Forest. "Novel and functionally selective 5-HT2C receptor agonist for treating Alcohol Use Disorder". RePORTER
List of investigational hallucinogens and entactogens
List_of_investigational_hallucinogens_and_entactogens
Chemical compound
agonists. The synthetic derivative RB-64 is notable because of its functional selectivity and potency. Salvinorin B methoxymethyl ether is seven times more
Salvinorin_A
Medical condition
Functional gastrointestinal disorders (FGID), also known as disorders of gut–brain interaction, include a number of separate idiopathic disorders which
Functional gastrointestinal disorder
Functional_gastrointestinal_disorder
Half maximal inhibitory concentration
obtaining 50% of a maximum effect in vivo. IC50 can be determined with functional assays or with competition binding assays. Sometimes, IC50 values are
IC50
Class of antidepressant medication
for inhibition of serotonin reuptake over norepinephrine reuptake. The selectivity ratios are approximately 1:30 for venlafaxine, 1:10 for duloxetine, and
Selective serotonin reuptake inhibitor
Selective_serotonin_reuptake_inhibitor
Protein-coding gene in the species Homo sapiens, named for ketazocine
Polepally PR, Brown PJ, et al. (January 2014). "Identification of novel functionally selective κ-opioid receptor scaffolds". Molecular Pharmacology. 85 (1): 83–90
Κ-opioid_receptor
Pharmaceutical compound
et al. (April 2025). "A cryptic pocket in CB1 drives peripheral and functional selectivity". Nature. 640 (8057): 265–273. Bibcode:2025Natur.640..265R. doi:10
VIP36
Chemical compound
xanomeline acts preferentially in the central nervous system as a functionally selective partial agonist at the M1 and M4 muscarinic receptors. It has more
Xanomeline
DNA sequences with no known biological function
Junk DNA (non-functional DNA) is a DNA sequence that has no known biological function. Most organisms have some junk DNA in their genomes—mostly pseudogenes
Junk_DNA
Class of chemical compounds
shared by all other related drugs and appear to be mediated by functionally selective serotonin 5-HT2A receptor activation. The anti-inflammatory effects
DOx
Dopamine receptor modulator
Stemp, G., & Routledge, C. (1999). A selective dopamine D 3 receptor antagonist, SB-269652, shows functional selectivity for D 3 receptors in vivo. Monitoring
SB269652
Class of transport proteins
essential for ion selectivity. They include the amino acid sequence (Thr-Val-Gly-Tyr-Gly) or (Thr-Val-Gly-Phe-Gly) typical to the selectivity filter of voltage-gated
Voltage-gated potassium channel
Voltage-gated_potassium_channel
FUNCTIONAL SELECTIVITY
FUNCTIONAL SELECTIVITY
Boy/Male
French
Fictional swordsman: (ambitious and filled with religious aspirations) from Alexander Dumas's...
Male
Egyptian
, an Egyptian functionary.
Boy/Male
Australian, French
Fictional Swordsman; Ambitious and Filled with Religious Aspirations; From Alexander Dumas's Three Musketeers
Boy/Male
English
The fictional character Jorel father of Superman.
Male
Egyptian
, a high Egyptian functionary.
Biblical
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Male
Egyptian
, a great functionary.
Boy/Male
English
The fictional character Jorel father of Superman.
Boy/Male
English
Modern. The fictional character Jorel father of Superman.
Male
Egyptian
, Functionary of the Interior.
Male
Egyptian
, the son of the functionary Heknofre.
Boy/Male
American, Australian, British, English, French
Mighty Spearman; The Fictional Character Jorel Father of Superman
Surname or Lastname
English
English : nickname from the animal, Middle English catte ‘cat’. The word is found in similar forms in most European languages from very early times (e.g. Gaelic cath, Slavic kotu). Domestic cats were unknown in Europe in classical times, when weasels fulfilled many of their functions, for example in hunting rodents. They seem to have come from Egypt, where they were regarded as sacred animals.English : from a medieval female personal name, a short form of Catherine.Variant spelling of German and Dutch Katt.
Boy/Male
American, Australian, British, Danish, English, Finnish, French, German, Scandinavian
Farmer; The Fictional Character Jorel Father of Superman; Earth Worker
Male
Egyptian
, an Egyptian functionary.
Male
Celtic
, great justiciary, or functionary.
Boy/Male
English
The fictional character Jorel father of Superman.
Boy/Male
American, British, English
Mighty Spearman; The Fictional Character Jorel Father of Superman
Boy/Male
American, British, English
Mighty Spearman; One who Saves; The Fictional Character Jorel Father of Superman
Boy/Male
Buddhist, Indian, Japanese
Mysterious Function
FUNCTIONAL SELECTIVITY
FUNCTIONAL SELECTIVITY
Boy/Male
English
From the elfs home.
Boy/Male
Hindu, Indian
Principle
Boy/Male
Arabic, Muslim
Careful; Watchful
Girl/Female
Tamil
Star, The pleiades
Girl/Female
American, British, English
Flash of Lightning
Boy/Male
Arabic, Muslim
Servant of the Promoter / Expediter
Boy/Male
British, Christian, English, German, Norse, Teutonic
Divinely Good
Boy/Male
Bengali, Gujarati, Hindu, Indian, Indonesian, Kannada, Malaysian, Sindhi, Tamil, Telugu, Thai, Traditional
Respect; God; Richness; Loyal
Male
English
English form of Roman Latin Livius, possibly LIVY means "bluish."
Girl/Female
German
From the Old German name Frithuric, meaning peaceful ruler.
FUNCTIONAL SELECTIVITY
FUNCTIONAL SELECTIVITY
FUNCTIONAL SELECTIVITY
FUNCTIONAL SELECTIVITY
FUNCTIONAL SELECTIVITY
adv.
In a functional manner; as regards normal or appropriate activity.
n.
A quantity so connected with another quantity, that if any alteration be made in the latter there will be a consequent alteration in the former. Each quantity is said to be a function of the other. Thus, the circumference of a circle is a function of the diameter. If x be a symbol to which different numerical values can be assigned, such expressions as x2, 3x, Log. x, and Sin. x, are all functions of x.
n.
One charged with the performance of a function or office; as, a public functionary; secular functionaries.
n.
The office, duties, or functions of a minister, servant, or agent; ecclesiastical, executive, or ambassadorial function or profession.
v. i.
To execute or perform a function; to transact one's regular or appointed business.
v. t.
To supply with an organ or organs having a special function or functions.
a.
Pertaining to, or connected with, a function or duty; official.
a.
Of or pertaining to fractions or a fraction; constituting a fraction; as, fractional numbers.
a.
Capable of, or pertaining to, flection or inflection.
n.
A derived function; a function obtained from a given function by a certain algebraic process.
pl.
of Functionary
n.
Paper fractional currency.
v. i.
Alt. of Functionate
a.
Pertaining to, or characterized by, fiction; fictitious; romantic.
a.
Relating to friction; moved by friction; produced by friction; as, frictional electricity.
n.
An angle upon which the value of some function depends; -- a term used more especially in connection with elliptic functions.
a.
Pertaining to the function of an organ or part, or to the functions in general.
a.
Relatively small; inconsiderable; insignificant; as, a fractional part of the population.
a.
Fractional.
n.
The appropriate action of any special organ or part of an animal or vegetable organism; as, the function of the heart or the limbs; the function of leaves, sap, roots, etc.; life is the sum of the functions of the various organs and parts of the body.