guanethidine
Trade name: ismelin
Small moleculeapproved
Approved
Jul 5, 1960
Guanethidine belongs to the general class of medicines called antihypertensives. It was used to treat high blood pressure (hypertension). It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues. It is taken up by norepinephrine transporters. It becomes concentrated in NE transmitter vesicles, replacing NE in these vesicles. — NCATS
Clinical trial activity
0 trials · 0 clinical orgs · 2 marketing orgs
Phase 1
0
Phase 2
0
Phase 3
0
Phase 4
0
Timeline
Indications
Approved for
Mechanism of action
- Norepinephrine transporterSUBSTRATE
SLC6A2 substrate
Taken up by transporter and displaces NE from vesicles
Combination products
esimil
with hydrochlorothiazide
Approval history
- approvedPriority reviewJul 5, 1960
Chemistry & pharmacology
Loading structure…
SMILES
N=C(N)NCCN1CCCCCCC1- Mol. weight
- 198.31 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL765 ↗
- WikipediaGuanethidine ↗
- NCATS5UBY8Y002G ↗
- ChEMBLCHEMBL2051958 ↗
- ChEMBLCHEMBL1345 ↗
Also known as
- 2-(1'-azacyclooctyl)ethylguanidine
- 2-(1'-azacyclooctyl)ethylguanidine
- 2-(1-n,n-heptamethyleneimino)ethylguanidine
- 2-(1-n,n-heptamethyleneimino)ethylguanidine
- (2-(hexahydro-1(2h)-azocinyl)ethyl)guanidine
- (2-(hexahydro-1(2h)-azocinyl)ethyl)guanidine
- (2-(octahydro-1-azocinyl)ethyl)guanidine
- (2-(octahydro-1-azocinyl)ethyl)guanidine
- abapresin
- azocine, 1-(2-guanidinoethyl)octahydro-
- azocine, 1-(2-guanidinoethyl)octahydro-
- esimil
- esimil
- ganda
- ganda
- guanethidine
- guanethidine
- guanethidine
- guanethidine
- guanethidine
- guanethidine
- guanethidine
- guanethidine
- guanethidine
- guanethidine
- guanéthidine
- guanéthidine
- guanethidine monosulfate
- guanethidine monosulfate
- guanethidine monosulfate
- guanethidine monosulfate
- guanethidine sulfate
- guanethidinum
- guanethidinum
- guanetidina
- guanetidina
- guanidine, (2-(hexahydro-1(2h)-azocinyl)ethyl)-
- guanidine, (2-(hexahydro-1(2h)-azocinyl)ethyl)-
- heptamethylenimine, 1-(2-guanidinoethyl)-
- heptamethylenimine, 1-(2-guanidinoethyl)-
- ismelin
- ismelin
- ismelin
- ismelin
- ismeline
- lotens
- n-(2-perhydroazocin-1-ylethyl)guanidine
- n-(2-perhydroazocin-1-ylethyl)guanidine
- octatensine
- oktatensin
Organizations
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Novartis | For profit | NDA2 | Jul 5, 1960 |
| Novartis | For profit | NDA | Jul 5, 1960 |
| Watson Pharmaceuticals | For profit | MKTG | — |