CLONIDINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C9H9Cl2N3
Molecular Weight	230.0941
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

c1cc(c(c(c1)Cl)NC2=NCCN2)Cl

InChI

InChIKey=GJSURZIOUXUGAL-UHFFFAOYSA-N

InChI=1S/C9H9Cl2N3/c10-6-2-1-3-7(11)8(6)14-9-12-4-5-13-9/h1-3H,4-5H2,(H2,12,13,14)

HIDE SMILES / InChI

Molecular Formula	C9H9Cl2N3
Molecular Weight	230.0941
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018891s028lbl.pdf
Curator's Comment:: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/017407s037lbl.pdf | https://clinicaltrials.gov/ct2/show/NCT02177461 | https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022331lbl.pdf | https://clinicaltrials.gov/ct2/show/NCT00556959

Clonidine is a centrally acting α2 adrenergic agonist and imidazoline receptor agonist used to treat high blood pressure, attention deficit hyperactivity disorder, anxiety disorders, tic disorders, withdrawal (from either alcohol, opioids, or smoking), migraine, menopausal flushing, diarrhea, and certain pain conditions. Clonidine treats high blood pressure by stimulating α2 receptors in the brain, which decreases peripheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic α2 receptors in the vasomotor center in the brainstem. This binding decreases presynaptic calcium levels, thus inhibiting the release of norepinephrine (NE). It has also been proposed that the antihypertensive effect of clonidine is due to agonism on the I1 receptor (imidazoline receptor), which mediates the sympatho-inhibitory actions of imidazolines to lower blood pressure. Clonidines mechanism of action in the treatment of ADHD is to increase noradrenergic tone in the prefrontal cortex (PFC) directly by binding to postsynaptic α2A adrenergic receptors and indirectly by increasing norepinephrine input from the locus coeruleus. Clonidine indicated in the treatment of hypertension. Clonidine hydrochloride tablets may be employed alone or concomitantly with other antihypertensive agents. The US Food and Drug Administration (FDA) has approved clonidine for the treatment of attention deficit hyperactivity disorder (ADHD), under the trade name of Kapvay alone or with stimulants in 2010, for pediatric patients aged 6–17 years.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Alpha-2a adrenergic receptor 62 Target ID: CHEMBL1867 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27265687	Partial Agonist 259		30.1999999999999993 nM [EC50]
Adrenergic receptor alpha-2 113 Target ID: CHEMBL2095158 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25521963	Partial Agonist 259	Opioid withdrawal Attention deficit hyperactivity disorder Hypertension	3.79999999999999982 nM [Ki]
Alpha-2b adrenergic receptor 27 Target ID: CHEMBL1942 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22750139	Partial Agonist 259		31.6000000000000014 nM [Ki]
Alpha-2c adrenergic receptor 37 Target ID: CHEMBL1916 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22750139	Partial Agonist 259		9.30000000000000071 nM [Ki]
Adrenergic receptor alpha-1 161 Target ID: CHEMBL2094251 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8784451	Partial Agonist 259	Hypertension Attention deficit hyperactivity disorder Opioid withdrawal	290 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/017407s037lbl.pdf	Primary	Adrenergic receptor alpha-2 Adrenergic receptor alpha-1	Approved 7997	CATAPRES-TTS-1 Approved Use INDICATIONS & USAGE Clonidine hydrochloride tablets, USP are indicated in the treatment of hypertension. Clonidine hydrochloride tablets, USP may be employed alone or concomitantly with other antihypertensive agents. Launch Date 466214400000
Attention deficit hyperactivity disorder 63 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022331s013lbl.pdf	Primary	Adrenergic receptor alpha-2 Adrenergic receptor alpha-1	Approved 7997	KAPVAY Approved Use INDICATIONS AND USAGE. KAPVAY® is a centrally acting alpha2-adrenergic agonist indicated for the treatment of attention deficit hyperactivity disorder (ADHD) as monotherapy or as adjunctive therapy to stimulant medications Launch Date 1254182400000
Opioid withdrawal 4 Sources: https://clinicaltrials.gov/ct2/show/NCT03174067	Primary	Adrenergic receptor alpha-2 Adrenergic receptor alpha-1	Phase IV 62	CATAPRES-TTS-1 Approved Use INDICATIONS & USAGE Clonidine hydrochloride tablets, USP are indicated in the treatment of hypertension. Clonidine hydrochloride tablets, USP may be employed alone or concomitantly with other antihypertensive agents. Launch Date 466214400000

C_max

Value	Dose	Co-administered	Analyte	Population
443 pg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022331s021lbl.pdf	0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered:		CLONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
7313 pg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022331s021lbl.pdf	0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered:		CLONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
12.57 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022331s021lbl.pdf	0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered:		CLONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

Doses

Dose	Population	Adverse events
0.25 mg 2 times / day multiple, oral Studied dose Dose: 0.25 mg, 2 times / day Route: oral Route: multiple Dose: 0.25 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, 13 years Health Status: unhealthy Age Group: 13 years Sex: M Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	Other AEs: Suicide attempt... Other AEs: Suicide attempt Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
2 mg 3 times / day multiple, oral Highest studied dose Dose: 2 mg, 3 times / day Route: oral Route: multiple Dose: 2 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/5454324/	unhealthy, adult Health Status: unhealthy Age Group: adult Sources: https://pubmed.ncbi.nlm.nih.gov/5454324/	Sources: https://pubmed.ncbi.nlm.nih.gov/5454324/
0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 10 years Health Status: unhealthy Age Group: median age 10 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	Disc. AE: Bradyphrenia... AEs leading to discontinuation/dose reduction: Bradyphrenia (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
0.1 mg 2 times / day multiple, oral Recommended Dose: 0.1 mg, 2 times / day Route: oral Route: multiple Dose: 0.1 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 9 years Health Status: unhealthy Age Group: median age 9 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	Disc. AE: Somnolence, Fatigue... AEs leading to discontinuation/dose reduction: Somnolence (3.9%) Fatigue (2.6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 9 years Health Status: unhealthy Age Group: median age 9 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	Disc. AE: Somnolence, Fatigue... AEs leading to discontinuation/dose reduction: Somnolence (6.4%) Fatigue (5.1%) Constipation (1.3%) Vomiting (1.3%) Electrocardiogram QT prolonged (1.3%) Rash (1.3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
0.1 mg 2 times / day steady, oral Dose: 0.1 mg, 2 times / day Route: oral Route: steady Dose: 0.1 mg, 2 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT00884832	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT00884832	Other AEs: Dry mouth, Drowsiness... Other AEs: Dry mouth (below serious, 16 patients) Drowsiness (below serious, 5 patients) Lightheadedness (below serious, 6 patients) Fatigue (below serious, 8 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT00884832

AEs

AE	Significance	Dose	Population
Suicide attempt		0.25 mg 2 times / day multiple, oral Studied dose Dose: 0.25 mg, 2 times / day Route: oral Route: multiple Dose: 0.25 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, 13 years Health Status: unhealthy Age Group: 13 years Sex: M Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
Bradyphrenia	1% Disc. AE	0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 10 years Health Status: unhealthy Age Group: median age 10 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
Fatigue	2.6% Disc. AE	0.1 mg 2 times / day multiple, oral Recommended Dose: 0.1 mg, 2 times / day Route: oral Route: multiple Dose: 0.1 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 9 years Health Status: unhealthy Age Group: median age 9 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
Somnolence	3.9% Disc. AE	0.1 mg 2 times / day multiple, oral Recommended Dose: 0.1 mg, 2 times / day Route: oral Route: multiple Dose: 0.1 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 9 years Health Status: unhealthy Age Group: median age 9 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
Constipation	1.3% Disc. AE	0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 9 years Health Status: unhealthy Age Group: median age 9 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
Electrocardiogram QT prolonged	1.3% Disc. AE	0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 9 years Health Status: unhealthy Age Group: median age 9 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
Rash	1.3% Disc. AE	0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 9 years Health Status: unhealthy Age Group: median age 9 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
Vomiting	1.3% Disc. AE	0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 9 years Health Status: unhealthy Age Group: median age 9 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
Fatigue	5.1% Disc. AE	0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 9 years Health Status: unhealthy Age Group: median age 9 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
Somnolence	6.4% Disc. AE	0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf	unhealthy, median age 9 years Health Status: unhealthy Age Group: median age 9 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022331Orig1s001.pdf
Dry mouth	below serious, 16 patients	0.1 mg 2 times / day steady, oral Dose: 0.1 mg, 2 times / day Route: oral Route: steady Dose: 0.1 mg, 2 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT00884832	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT00884832
Drowsiness	below serious, 5 patients	0.1 mg 2 times / day steady, oral Dose: 0.1 mg, 2 times / day Route: oral Route: steady Dose: 0.1 mg, 2 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT00884832	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT00884832
Lightheadedness	below serious, 6 patients	0.1 mg 2 times / day steady, oral Dose: 0.1 mg, 2 times / day Route: oral Route: steady Dose: 0.1 mg, 2 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT00884832	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT00884832
Fatigue	below serious, 8 patients	0.1 mg 2 times / day steady, oral Dose: 0.1 mg, 2 times / day Route: oral Route: steady Dose: 0.1 mg, 2 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT00884832	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT00884832

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1470	substrate 865	substrate 1038	inhibitor 1360

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1089 OCT1 473 L-type Ca2+ channels 25 K+ channels 50	CYP1A2 892 CYP1A1 302 CYP3A5 346 CYP2A6 452 CYP2B6 575 CYP2C8 586 CYP2C18 143 CYP2C19 830 CYP2E1 567 CYP2J2 51 CYP1B1 82

Drug as perpetrator

Target	Modality	Activity
P-gp 1255	inhibitor 2614 Sources: https://www.sciencedirect.com/science/article/abs/pii/0006291X9091939P Page: 265	likely
L-type Ca2+ channels 27	inhibitor 2614 Sources: https://www.sciencedirect.com/science/article/abs/pii/S0006899300025920 Page: abstract	no
K+ channels 50	inhibitor 2614 Sources: https://journals.lww.com/anesthesia-analgesia/Fulltext/2011/12000/Molecular_Mechanisms_of_the_Inhibitory_Effects_of.14.aspx Page: abstract	yes [IC50 1.21 uM]
OCT1 488	inhibitor 2614 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3129651/ Page: 3	yes

Drug as victim

Target	Modality	Activity
CYP1B1 82	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: 1	no
CYP2A6 452	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: 1	no
CYP2B6 575	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: 1	no
CYP2C18 143	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: 1	no
CYP2C19 830	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: 1	no
CYP2C8 586	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: 1	no
CYP2C9 865	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: 1	no
CYP2E1 567	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: 1	no
CYP2J2 51	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: 1	no
CYP1A1 302	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: abstract	yes
CYP1A2 892	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: abstract	yes
CYP2D6 1038	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: abstract	yes
CYP3A4 1470	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: abstract	yes
CYP3A5 346	substrate 2752 Sources: https://dmd.aspetjournals.org/content/38/9/1393.short Page: abstract	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1392	inhibitor 1374 Sources: https://www.sciencedirect.com/science/article/abs/pii/S1056871907002808 Page: 102

Sourcing

Vendor/Aggregator	ID	URL
1PlusChem LLC	1P00I8MT
A2B Chem	AI50197
A2Z Synthesis	A2Z00085415
AA Blocks	AA00I83D
ACT Chemical	ACT05586
AK Scientific	H535
AK Scientific	J10306
APExBIO	B1333
AbovChem LLC	HY-B0409A
Alfa Chemistry	ACM4205907
Angene	AGN-PC-0W1557
Angene	AGN-PC-0WAJ74
Aronis	BBC/149
Aronis	BBC/509
BOC Sciences	4205-90-7
BOC Sciences	4205-91-8
BioSynth	Q-200881
BlocksMatrix Scientific	147891
BlocksMatrix Scientific	58273
Bosche Scientific	C0205
Bosche Scientific	C18899
Capot Chemical	20363
Cayman Chemical	15949
Chem Scene	CS-0012297
Chem Scene	CS-2509
ChemShuttle	113823
Combi-Blocks	OR-1592
Compound Cloud	20179
Compound Cloud	2803
Compound Cloud	BCC0065844
Enamine	BBV-40197751
Enamine	BBV-93049830
Enamine	EN300-119527
Fluorochem	358090
Fluorochem	393321
Frontier Scientific Services	100076169
Hairui	HR135273
Hairui	HR137391
Hangzhou APIChem Technology	AC-10306
Hangzhou Yuhao Chemical Technology	RT2573
HongKong Chemhere	SCA32582
Innovapharm	BBS-00028806
KeyOrganics	KS-1253
Lab Network	LN00326971
Lab Network	LN01273348
Lab Seeker	SC-16715
Lab Seeker	SC-47255
MedChem Express	HY-B0409A
MolPort	MolPort-001-684-471
MolPort	MolPort-003-928-972
MolPort	MolPort-016-578-933
Molnova	M14433
MuseChem	R006717
MuseChem	R023441
Norris Pharm	NSZB-A092098
Otava	6057088
PI Chemicals	PI-13782
Princeton BioMolecular Research	OSSL_790092
Princeton BioMolecular Research	PBMR215359
Scientific Exchange	R-035309
Scientific Exchange	Z-033248
Selleck Chemicals	S2458
ShangHai Biochempartner	BCP07223
ShangHai Biochempartner	BCP14375
Sigma Aldrich	1140407
Sigma Aldrich	1140407\|USP
Sigma Aldrich	27545
Sigma Aldrich	27545\|SIAL
Sigma Aldrich	B001
Sigma Aldrich	B001\|SIGMA
Sigma Aldrich	BP085
Sigma Aldrich	BP085\|SIAL
Sigma Aldrich	C-033
Sigma Aldrich	C-033\|CERILLIAN
Sigma Aldrich	C2400000
Sigma Aldrich	C2400000\|SIAL
Sigma Aldrich	C7897
Sigma Aldrich	C7897\|SIGMA
StruChem	SC-16715
StruChem	SC-47255
TargetMol	T1247
TargetMol	T7045
Tetrahedron	TS30349
TimTec	SBB003065
TimTec	ST088475
Tocris	690
Toronto Research Chemicals	C587120
Toronto Research Chemicals	C587130
Vesino Industrial Co Ltd	VA10617
Vitas-M Laboratory	BBL025137
Vitas-M Laboratory	STL355995
W&J PharmaChem	100197
W&J PharmaChem	50C529033
Wonderchem	WD0641R
ZINC	ZINC000000896484	http://zinc15.docking.org/substances/ZINC000000896484
eMolecules	192738993
eMolecules	29542544
eMolecules	300021863
eMolecules	31261419
eMolecules	493859
eMolecules	901678
eMolecules	969274
eNovation Chemicals	D588579
mcule	MCULE-5017779690
mcule	MCULE-6555265624
mcule	MCULE-9274594116

PubMed

Title	Date	PubMed
Sexual dysfunction related to antihypertensive agents: results from the animal model.	1999 Apr	10356671
Cocaine-induced hypertension: role of the peripheral sympathetic system.	1999 Aug	10433872
Scopolamine-induced convulsions in food given fasted mice: effects of clonidine and tizanidine.	1999 Jun	10372568
Alpha-2 adrenergic receptor agonists block stress-induced reinstatement of cocaine seeking.	2000 Aug	10882840
Low-dose clonidine and neostigmine prolong the duration of intrathecal bupivacaine-fentanyl for labor analgesia.	2000 Feb	10691221
[Clonidine hallucinations: description of a clinical case].	2000 Jan-Feb	10822881
The influence of indomethacin on the acth secretion induced by central stimulation of adrenergic receptors.	2000 Jun	10898105
Hypertensive crisis and myocardial infarction following massive clonidine overdose.	2000 May	10852088
Optimal dose of intrathecal clonidine added to sufentanil plus bupivacaine for labour analgesia.	2000 Sep	10989857
P75-expressing elements are necessary for anti-allodynic effects of spinal clonidine and neostigmine.	2001	11226704
Oops--wrong dose of epidural clonidine in children!	2001 Apr	11300396
Alpha2 adrenergic receptors and the central control of breathing in the cane toad, Bufo marinus.	2001 Apr	11282388
Baclofen versus clonidine in the treatment of opiates withdrawal, side-effects aspect: a double-blind randomized controlled trial.	2001 Feb	11286609
The use of baclofen in cluster headache.	2001 Feb	11252142
Mortality after coronary artery occlusion in different models of cardiac hypertrophy in rats.	2001 Feb	11230273
Characterization of adenylyl cyclases in cultured human granulosa cells.	2001 Feb	11226046
Effectiveness of apraclonidine 1% in preventing intraocular pressure rise following macular hole surgery.	2001 Feb	11159479
Exercise attenuates alpha-adrenergic-receptor responsiveness in skeletal muscle vasculature.	2001 Jan	11133908
A comparison of oral clonidine and oral midazolam as preanesthetic medications in the pediatric tonsillectomy patient.	2001 Jan	11133600
Use of trifluoroperazine isolates a [(3)H]Ifenprodil binding site in rat brain membranes with the pharmacology of the voltage-independent ifenprodil site on N-methyl-D-aspartate receptors containing NR2B subunits.	2001 Jan	11123375
Baclofen-impairment of memory retention in rats: possible interaction with adrenoceptor mechanism(s).	2001 Jan 12	11164386
Galanin/alpha2-adrenoceptor interactions in telencephalic and diencephalic regions of the rat.	2001 Jan 22	11201077
Clonidine-induced antinociception and locomotor hypoactivity are reduced by dexamethasone in mice.	2001 Mar	11291750
Noradrenergic modulation of calcium currents and synaptic transmission in the olfactory bulb of Xenopus laevis tadpoles.	2001 Mar	11285006
Antinociceptive interaction between spinal clonidine and lidocaine in the rat formalin test: an isobolographic analysis.	2001 Mar	11226110
The analgesic interaction between intrathecal clonidine and glutamate receptor antagonists on thermal and formalin-induced pain in rats.	2001 Mar	11226109
Neural circuits regulating pulsatile luteinizing hormone release in the female guinea-pig: opioid, adrenergic and serotonergic interactions.	2001 Mar	11207938

Patents

Sample Use Guides

In Vivo Use Guide

Oral

Route of Administration: Other

In Vitro Use Guide

Neural membranes (P2 fractions) were prepared from the prefrontal cortex of human brains obtained at autopsy. Specific Clonidine binding was measured in 0.55 mL aliquots (50 mM Tris HCl, pH 7.5) of the neural membranes, which were incubated with [3H]RX821002 (1 nM) for 30 min at 25 °C in the absence or presence of the Clonidine (10^-12 M to 10^-3 M, 10 concentrations). Specific binding was determined and plotted as a function of the compound concentration. Incubations were terminated by diluting the samples with 5 mL of ice-cold Tris incubation buffer (4 °C). Membrane-bound [3H]RX821002 was separated by vacuum filtration through Whatman GF/C glass fiber filters. Then the filters were rinsed twice with 5 mL of incubation buffer and transferred to minivials containing 3 mL of OptiPhase “HiSafe” II cocktail and counted for radioactivity by liquid scintillation spectrometry.

Substance Class	Chemical Created by `admin` on `Fri Jun 25 20:54:07 UTC 2021` Edited by `admin` on `Fri Jun 25 20:54:07 UTC 2021`
Record UNII	MN3L5RMN02
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CLONIDINE

Official Name

English

CLONIDINE [VANDF]

Common Name

English

CLONIDINE [WHO-DD]

Common Name

English

ST-155-BS

Code

English

CLONIDINE [HSDB]

Common Name

English

CLONIDINE [USP-RS]

Common Name

English

CLONIDINE EXTENDED RELEASE

Common Name

English

CLONIDINE [MI]

Common Name

English

CLONIDINE [USAN]

Common Name

English

CLONIDINE [JAN]

Common Name

English

CATARPRES-TTS

Brand Name

English

CLONIDINE [MART.]

Common Name

English

CLONIDINE [ORANGE BOOK]

Common Name

English

2-((2,6-DICHLOROPHENYL)IMINO)IMIDAZOLIDINE

Systematic Name

English

CLONIDINE [INN]

Common Name

English

CLONIDINE [USP MONOGRAPH]

Common Name

English

Classification Tree Code System Code

WHO-ATC

C02LC51